International Journal of Pharmacy and Pharmaceutical Sciences

Published by Innovare Academic Sciences
Online ISSN: 0975-1491
Print ISSN: 2656-0097
Publications
The purpose of the present research was to prepare and evaluate mannitol and cellulose based, directly compressible excipient using freeze-thawing technique. The mannitol to cellulose ratio (50:50, 60:40, and 70:30) and the rotation speed of propeller stirrer (200, 600, and 1000 rpm) were selected as independent variables in a 32 full factorial design. Water acted as a good medium for mannitol as well as a bridging liquid for agglomeration of mannitol with cellulose. The agglomerates were evaluated for percentage fines and carr’s index. Tablets were prepared on a rotary tablet press, and they were evaluated for friability, tensile strength, water absorption ratio, and disintegration time. Multiple linear regression analysis was carried out to evolve full and reduce models. The use of composite index was demonstrated for the selection of an appropriate batch. The optimized batch was characterized by different scanning calorimetry (DSC), scanning electron microscopy, Fourier Transform Infrared (FTIR) Spectral Study, granular friability, Kawakita’s equation, Kuno’s equation and Heckle equation. The results of dilution potential study reveal that up to 30% nimesulide, a poorly compressible drug and 50% metformin, a hygroscopic drug, can be incorporated in the co-crystallized product. The product was less sensitive to lubricant in lubricant sensitivity test. In conclusion, the properties of agglomerated product, such as flowability, compactibility, and dissolution rate were improved profoundly using the developed technique resulting in successful direct tableting without need to additional process of physical blending of agglomerates.
 
The dried aerial parts of Phyla nodiflora Linn. were subjected to successive extraction using the solvents (Petroleum ether, chloroform, methanol and water) in increasing order of polarity. The prepared extracts were then subjected to preliminary phytochemical analysis. It was found that the plant possesses steroids, alkaloids, carbohydrates, flavonoids, essential oil, tannins and salts of potassium. The methanol and aqueous extracts were selected for further study. The diuretic potential of methanol and aqueous extracts of the aerial parts was assessed in albino rats using in-vivo Lipschitz test model. The volumes of urine, urinary concentration of sodium and potassium ions were the parameters of the study. Frusemide was used as standard. The results indicate that methanol and aqueous extract at 500 mg/kg body weight shows a significant (p<0.05) increase in the urine volume and electrolyte excretion (p<0.001) when compared to control. Both the extracts show significant diuretic activity. From the present study it may be concluded that the constituents present in methanol and aqueous extracts may be responsible for diuretic activity.
 
Diabetes mellitus constitutes a major health problem in modern societies. A major role of antidiabetic therapy is to restrict blood glucose control, which approximates normal fasting levels and normal elevations of postprandial blood glucose. Sulfonylureas are the mainstay of antidiabetic therapy for many years.The present work involves the synthesis of the lead molecule N-[4-{2-(5-chloro-2-methoxy benzamido) ethyl}phenyl sulfonyl]-N’-cyclohexyl urea known as Glibenclamide, second generation sulfonylurea and its novel analogs. The synthesized compounds were screened for antidiabetic activity .The structures of title compounds were established by elemental and spectral analysis.
 
Anthelmintic activities of aqueous and ethanolic extracts of fruits of plant Solanum surattense on indian earthworm Pheretima postuma. Each bar is represented as mean ± standard deviation (n = 5). Group I – Control (Normal saline water), group II – standard – 1 (Piperazine citrate), group III – standard – 2 (Albendazole), group IV to IX – Aqueous extract of dose 10, 15, 20, 25, 30 and 35 mg/ml respectively and group X to XVI – Ethanolic extract of dose 10, 15, 20, 25, 30 and 35 mg/ml respectively. 
Solanum surattense Linn is found in the tribal area of Koraput district and extensively used traditionally by the tribal people as anthelmintic, diuretic, antiarrhythmic, hypotensive, expectorant and carminative. The present study is an attempt to explore the anthelmintic activity of aqueous and ethanolic extract of fruits of plant Solanum surattense in a comparative study. The various doses of aqueous and ethanolic extracts were evaluated for their anthelmintic activities on adult Indian earthworms, Pheretima postuma. All extracts of both the solvent were able to show anthelmintic activity at 10 mg/ml concentration. The activities are well comparable with the standard drugs, Piperazine citrate and Albendazole. All the doses of aqueous and ethanolic extract of Solanum surattense showed better anthelmintic activity than the standard drugs. When the dose of the extract is increased, a gradual increase in anthelmintic activity was observed. Aqueous extract showed better anthelmintic activity in comparison to the ethanolic extract of Solanum surattense. The data were verified as statistically significant by using one way ANOVA at 5 % level of significance (p < 0.05).
 
The present study was carried out to evaluate the drug-drug interaction between antidiabetic drugs and antifungal drugs. Interaction of Pioglitazone and Rosiglitazone the known Thiazolidinedione antidiabetic drugs with Itraconazole (antifungal drug) was evaluated in alloxan induced diabetic rats. The blood samples were collected from diabetic rats at different time interval upto 24hrs and blood glucose was estimated. Itraconazole (18 mg/kg, p.o.) pretreatment has significantly altered the onset of antidiabetic effect of Pioglitazone from 22.70 % to 30.89 % and significantly enhanced the peak antidiabetic effect from 56.21 % to 68.30 %. Similarly pretreatment with Itraconazole (18 mg/kg, p.o) has also significantly altered the onset of antidiabetic effect of Rosiglitazone from 26.74 % to 30.07 % and enhanced the peak antidiabetic effect from 45.08 % to 58.50 %. Duration of antidiabetic effect was raised from more than 24hrs.This study indicates that Therapeutic drug monitoring has to be required to readjust the therapeutic dose of Itraconazole and Thiazolidinedione when they used concomitantly.
 
The present study was designed to investigate the anti-oxidant activity of the methanolic extract of Portulaca oleracea. The methanolic extract was evaluated by TLC and HPTLC fingerprint method. Anti-oxidant activity of methanolic extract was determined by DPPH free radical scavenging activity, reducing power by FeCl3, nitric oxide free radical scavenging activity, super oxide scavenging activity by alkaline DMSO method.
 
Structure of skin and mechanism of penetration into skin Need of penetration enhancement Penetration enhancement is the most critical factor in transdermal systems, so as to improve flux. Flux (J) can be defined as the amount (M) of material flowing through unit cross section (S) of a barrier in unit time (t). Flux can be given by: J=dM/S.dt 9. Each phase of the membrane can be characterized in terms of diffusional resistance(R), which usually is the function of thickness (hs) of the phase, the permeant diffusion coefficient (Ds) within the phase, and the partition coefficient (Ks) between the membrane phase and external phase.
Transdermal delivery of drugs through the skin to the systemic circulation provides a convenient route of administration for a variety of clinical indications. For transdermal delivery of drugs, stratum corneum is the main barrier layer for permeation of drug. So to circumvent the stratum corneum and to increase the flux through skin membrane, different approaches of penetration enhancement are used. Many reviews had described regarding the chemical penetration enhancement but vehicle based enhancement approach is not exploited for reviews. Drug-vehicle based enhancement methods such as drug selection, vesicles and particles, liposomes, prodrugs and ion-pairs, chemical potential of drug, eutectic systems, complexation are used in transdermal research as better alternative method to enhance permeation of drugs through skin. The review presents mainly the routes of penetration through skin and the approaches of drug-vehicle interaction based enhancement to optimise the transdermal delivery system.
 
Spectra of Itopride hydrochloride
A simple, precise economical and fast visible spectrophotometric method has been developed for the determination of Itopride hydrochloride in tablet dosage form. Developed is based on formation of extractable colored complex of drug with coloring agent mordant blue 3. A wavelength maximum was found to 471.0 nm. Linearity was observed 30-70 mg/mL The proposed method describes the determination of Itopride hydrochloride by visible spectrophotometric method which is a precise and selective. The result of analysis have been validated statistically and also by recovery studies.
 
Thiazolidinone, a saturated form of thiazole with carbonyl group on fourth carbon, has been considered as a magic moiety (wonder nucleus) which posses almost all types of biological activities. This diversity in the biological response profile has attracted the attention of many researchers to explore this skeleton to its multiple potential against several activities. Present article is sincere attempt to review chemistry, synthesis, spectral studies and applications of 4-thiazolidinone.
 
In vitro release profile of various haloperidol formulations  
shows that all the formulated
The purpose of this investigation was to develop fast dissolving tablets of haloperidol using camphor as a subliming agent. Orodispersible tablets of haloperidol were prepared by wet granulation technique using camphor as subliming agent and sodium starch glycolate together with crosscarmellose sodium as superdisintegrants. Camphor was sublimed from the granules by exposing the granules to vacuum. The porous granules were then compressed in to tablets. Alternatively, tablets were first prepared and later exposed to vacuum. The formulations were evaluated for weight variation, hardness, friability, drug content, wetting time, in vitro and in-vivo dispersion, mouth feel and in vitro dissolution. All the formulations showed low weight variation with dispersion time less than 45 seconds and rapid in vitro dissolution. Sublimation of camphor from tablets resulted in superior tablets as compared with the tablets prepared from granules that were exposed to vacuum. The results revealed that the tablets containing subliming agent had a good dissolution profile. The drug content of all the formulations was within the acceptable limits of the United States Pharmacopoeia XXVII. The optimized formulation showed good release profile with maximum drug being released at all time intervals. It was concluded that fast dissolving tablets with improved haloperidol dissolution could be prepared by sublimation of tablets containing suitable subliming agent. This work helped in understanding the effect of formulation processing variables especially the subliming agent on the drug release profile. The present study demonstrated potentials for rapid absorption, improved bioavailability, effective therapy and patient compliance.
 
Present investigation describes preparation of microspheres by solvent evaporation and W/O emulsion solvent evaporation methods followed by in vitro characterization of microspheres to evaluate the effect of method of preparation on physical properties and drug release profile of microspheres. The microspheres were found to be discrete, spherical with free flowing properties. The morphology (Scanning Electron Microscopy), particle size distribution, entrapment efficiency and their release profiles were investigated. The yield was found to be maximum in case of solvent evaporation method. The mean geometric particle size of microspheres prepared by solvent evaporation method was found in the ranges of 40-50 µm and the microspheres prepared by W/O emulsion solvent evaporation method was found in a ranges of 126-150 µm, respectively. The microcspheres formulation prepared by solvent evaporation method has shown greater encapsulation efficiency than W/O emulsion solvent evaporation method. The drug carrier interactions were investigated in solid state by Fourier Transform Infrared (FT-IR) spectroscopy study. In vitro drug release rate for microspheres was found to be sustained over 8 hours. Hence, it can be concluded that the formulation prepared by solvent evaporation method, has potential to deliver Losartan potassium in a controlled manner in a regular fashion over extended period of time in comparison to all other formulations and can be adopted for a successful oral delivery of Losartan potassium for safe management of hypertension. All data are verified as statistically significant by using one way ANOVA at 5 % level of significance (p < 0.05).
 
The effect of ibuprofen – an anti-inflammatory, analgesic drug was tested on pregnant females at different developmental phases. The fetus was collected on 12th, 15th and 18th gestation days (gd). Embryos on the day of parturition and 5 day old new born were considered for experimental study. Ovary and uterus of the mother was also taken into account for histopathological examination. The adverse effects on pregnancy outcome included a significant reduction in the number of implantation and significant increase in percentage of post implantation loss. The body weight as well as physical characteristics varied due to the treatment at different phases of gestation. The concentrations of brain DNA and RNA of the fetus and the pups were also lower compared to controls. A major change in the histological architecture was seen in the sections of ovary and uterus of the mother. These findings suggest the susceptibility of the drug to the mother as well as to the embryo.
 
Phosphodiesterase enzyme inhibitors like Sildenafil citrate and tadalafil has revolutionised the treatment of erectile dysfunction. Priapism as a side effect of Sildenafil has been reported very rarely. We report a case of priapism caused by usual dose of Sildenafil
 
The approach to new drugs through natural products has proved to be the single most successful strategy for the discovery of new drugs, but in recent years its use has been deemphasized by many pharmaceutical companies in favor of approaches based on combinatorial chemistry and genomics, among others. Again with rapid industrialization of the planet and the loss of ethnic culture and customs, some of the information on ethnomedicine will no doubt disappear. An abundance of ethnomedical information on plant uses can be found in scientific literature but has not yet been compiled into a usable form. Collection of ethnomedical information especially in the developing countries remains primarily an academic endeavour of little interest to most industrial groups. This article reviews some of the past successes of the natural products approach and also explores some of the reasons why it has fallen out of favor among major pharmaceutical companies and the challenges in drug discovery from Natural Products especially Higher Plants. In this review we consider the past, present, and future value of employing information from plants used in traditional medical practices (ethnomedicine) for the discovery of new bioactive compounds.
 
Ex vivo permeation of zolmitriptan from buccal patches (F10- F12) 
Ex vivo Release of zolmitriptan from formulations
In the present study, buccal patches of zolmitriptan were formulated by solvent casting method using HPMC E 15, aloe vera, Na CMC and eudragit RS100 as film forming polymers. The developed patches were evaluated for the thickness, folding endurance, bioadhesion strength, in-vitro residence time, mucoadhesive strength, in vitro drug release studies and ex-vivo drug permeation characteristics. Formulation F10 (contains HPMC E 15 & eudragit RS 100) has shown optimum ex-vivo mucoadhesion strength (19.4±0.9 g), in vitro residence time (6.0±0.14 hrs), in vitro drug release (75.06±1.12%) for 8hrs and satisfactory surface PH (6.8±0.02), ex vivo drug permeation (94.04±1.04%). The IR spectroscopic studies revealed that there is no evidence for chemical interaction between drug and polymers.
 
p> Objective: This work was undertaken with the aim of isolating and screening fungal soil isolates with fibrinolytic activity. Methods: Soil sample near slaughter house was collected and screened for fibrinolytic activity by using fibrin-agar. Enzyme production was optimized under various parameters like pH, temperature, substrate concentration and purified partially by ammonium sulphate precipitation. The stability of the partially purified enzyme was analyzed under the influence of a wide range of pH, temperature, and substrate concentrations. Results: Among the seven isolates screened, Aspergillus carbonarius S-CSR-0007 exhibited largest clear zone and was selected for further studies. Among the various substrates tested casein was found to support the highest caseinolytic activity of 816 U/ml and fibrinolytic activity of 510 U/ml. The culture supernatant of A. carbonarius S-CSR-0007 was fractionated by ammonium sulfate precipitation followed by dialysis, and maximum activity was obtained in the fraction with 80% ammonium sulfate, with an enzyme activity of 1200 U/ml using tyrosine as standard. The partially purified fibrinolytic enzyme showed optimal activity at 45 °C and pH 7.0. The enzyme was stable up to a temperature of 50 °C and pH 8.0, and the optimum substrate concentration was 4%. Conclusion: The crude enzyme showed high blood clot lysis activity, which may be a good candidate in the pharmaceutical industry. However, more studies need to be carried out to establish its clinical use.</p
 
D-002, a mixture of six higher aliphatic primary alcohols from beeswax, has been shown to produce gastroprotective effects mediated by increased gastric mucus secretion, improved mucus composition, and the reduction of lipid peroxidation. D-002 is able to heal acetic acid-induced gastric ulcers in rats, but its effects on this model had not been compared with those of proton pump inhibitors (PPI) or histamine 2-receptor (H2RA). This study compared the effects of D-002, omeprazole, and ranitidine on acetic acid-induced gastric ulcers in the rat, and on the associated neutrophil infiltration and angiogenesis in the ulcerated areas. Rats were randomized into eight groups: a vehicle control and seven with acetic acid-induced ulceration: a positive control, two D-002 (200 and 400 mg/kg, respectively), two omeprazole (5 and 10 mg/kg), and two ranitidine (25 and 50 mg/kg) groups. Gastric ulcers were produced by serosal application of acetic acid. Ulcer indexes and histological assessment were done. Significant reductions of ulcer indexes were seen with D-002 (200 and 400 mg/kg) (49% and 60%, respectively), omeprazole (5 and 10 mg/kg) (39% and 61%), and ranitidine (25 and 50 mg/kg) (52% and 68%). All treatments reduced ulcer sizes and inflammatory infiltrates, with signs of re-epithelization, both groups of D-002 and the highest dose of omeprazole showed the greatest effect on angiogenesis. Concluding, at the doses tested, D-002 healed acetic acid-induced ulcers as effectively as omeprazole and ranitidine, an effect associated to the reduction of neutrophil infiltration and to the increase of restorative angiogenesis into the ulcerated areas.
 
Gelucires (54/02, 43/01) have been used in preparation of floating sustained release formulations to prolong gastric residence time and increase its bioavailability. In this type of formulations Methocel K100M CR has been used as a swelling as well as a release-retarding polymer. The objective of this study was to explore the application of Gelucire 39/01 for the design of sustained release multi-unit and single-unit floating systems of metronidazole. Metronidazole-Gelucire 39/01 granules were prepared by melt granulation technique, alone and after addition of hydroxypropylmethylcellulose K15M (HPMC) or sodium cross-linked carboxymethylcellulose (Carmacel). The formulations were evaluated in vitro for their floating ability and drug release. Increasing proportions of Gelucire decrease the initial fast release of the drug that stabilizes and practically come to an end thereafter. The granules floating times were greater than 6 hours. The addition of HPMC and Carmacel increase the drug release that stabilizes after 2 hours. The use of single-unit systems (tablets) allowed a more gradual drug release. Carmacel formulations showed a span of drug dissolved after 3 hours ranging from 20 mg to 495 mg, with a trend to stabilize after 3 hours while HPMC formulations showed a range from 16 mg to 156 mg and a trend to increase the drug release. HPMC tablets floated more than 3 hours while Carmacel tablets showed no floatability. Gelucire 39/01, can be considered as a carrier for design of floating drug delivery systems only when mixed with dissolution enhancers that increase the permeability of the almost impermeable wax matrix.
 
The persistence and continuous application of these synthetic pyrethroids may create a problem directly or indirectly in the higher tropical level of the ecosystem. Accidental exposure at the work place and their presence in the environment has aroused concern over their possible adverse effects on human health. Toxic effect of sub chronic and acute dose exposure of a synthetic pyrethroid, Cyfluthrin under the trade name Solfac 050EW, on the serum aminotransferase were observed in this study. Oral administration of sub-chronic dose (one-fourth of the recommended dose) of Cyfluthrin for 15 days and 30 days showed significant increase in Alanine transaminase (ALT) content and Aspartate transaminase (AST) content as compared to control group. For acute studies (double the recommended dose), after oral administration of Cyfluthrin for 3 hrs, 24 hrs and 15 days, a highly significant increase in content of ALT and AST was observed as compared to control group. The present study suggests that Cyfluthrin (Solfac 050EW) shows significant toxic effects on serum aminotransferase of Swiss Albino Mice.
 
Standardization of phytopharmaceuticals are much needed to authenticate by natural or others scientific means therefore, in this research we performed pharmacognostic studies of four herbs Trigonella foenum graecum L.(1), Azadirachta indica L.(2), Psoralea corylifolia L.(3), Punica granatum L.(4) and two minerals red ochre (5) and purified sulphur (6) for herbomineral formulation (ALG-O6) to cure vitiligo. Fresh or dried seeds of all these herbs as well as their powdered samples were studied according to micro morphological, anatomical and histological aspects by using various chemical reagents. The common characteristic features of the sample herbs were parenchyma and sclerenchymatous cells were present in Azadirachta indica L., Punica granatum L. and Trigonella foenum graecum L., oil cells were seen in Azadirachta indica L. (large thin walled) and Psoralea corylifolia L. (medium thick walled), Ca oxalate crystals prism like were present in Azadiracta indica L. and both types prism and cluster were seen in Punica granatum L. along with abundant tannin containing cells while thickly lignified cells, fusiform, mucilage and color containing cells were present in both Azadirachta indica L. and Trigonella foenum graecum L. respectively. Mineral drugs after cleaning and purification were organoleptically standardized through sensory method (color, odor and taste).
 
Objective: Chitinase plays an important role against fungal pathogen and is a hopeful solution against fungal diseases. The main of this research is to screen a chitin degrading strain which can significantly used as biocontrol agent against Fusarium oxysporum. Methods: In the present study, chitinase producing bacteria were isolated from soil sample of crop field and identified based on biochemical observation and 16S rRNA analysis. The molecular weight of the enzyme was determined by zymogram. The purified enzyme from identified strain JD-09 was tested for antagonistic activity against Fusarium oxysporum. Results: Strain JD-09 was screened and identified as Bacillus subtilis. The strain exhibited a maximum chitinase production of 1.33 U/mL in colloidal chitin broth after 3 days of cultivation at 28 °C. The molecular weight of the chitinase was estimated to be 57 kDa, 39 kDa and 30.7 kDa. Hydrolysis products of the fungal cell wall by the purified enzymes of B. subtilis JD-09 were analyzed by high-pressure liquid chromatography (HPLC) and identified as oligosaccharides. Conclusion: It can be interfered that Bacillus subtilis JD-09 may be an optimal candidate for use as an antifungal agent of Fusarium wilt in crops. The purified chitinase can be directly applied for suppressing growth of living fungal hyphae.
 
Mean relative percentage inhibition of compounds
p> Objective: The objective of this research was to synthesize and evaluate anti-microbial properties of 1-(6-nitro-2 H -benzo[ b ][1,4]thiazine-3(4 H )-ylidene)hydrazine-1,1-dioxide derivatives. Methods: These new compounds were synthesized by reaction of 2 H -benzo[b][1,4]thiazin-3(4 H )-one with hydrazine derivatives and oxidized at the sulfur atom by 30% hydrogen peroxide to obtain sulfones. All the synthesized compounds were evaluated for antimicrobial activity using the disc diffusion method. Results: The FTIR, <sup>1</sup>HNMR, <sup>13</sup>CNMR and Mass studies confirms the synthesis of some new 1-(6-nitro-2 H -benzo[ b ][1,4]thiazine-3(4 H )-ylidene) hydrazine-1,1-dioxide derivatives. Compound 5f showed potent antimicrobial activity whereas compounds 5c and 5e showed moderate antimicrobial activity. Conclusion: Result obtained in this research work clearly indicated that the compound 5f having methyl at 2 position and nitro groups at 2′ and 4′ position showed the most potent antimicrobial activity. </p
 
Objective: To synthesize and study the docking pattern and Anti inflammatory activities of some new analogues of Imidazo [1, 2-a] pyridines. Methods: A scheme involving the synthesis of a modern series of ten substituted 5-(2-Methyl imidazo [1, 2-a] pyridine-3- yl) -2, 5 -dihydro -1, 3, 4- thiadiazol-2-amines (6a- j) using 2-amino pyridine 1 as the starting material, through an order of four reactions was proposed. The derivatives were subjected to docking studies using the protein sequences for prostaglandin reductase. It was found that all the synthesized derivatives possessed very good binding energy, bringing into consideration that, the compounds are good inhibitors of prostaglandin reductase and hence are vested with anti-inflammatory properties. The scheme was then practically preceded and the synthesized compounds were characterized based on spectral data and elemental analysis. The new moieties were then evaluated for invitro anti-inflammatory property by Human Red Blood cell (HRBC) membrane stabilization method using Diclofenac as the standard drug. Results: All the compounds synthesized showed inhibition of inflammation out of which compounds 6a, 6b, 6c & 6f possessing meta nitro, para nitro, meta hydroxy and trimethoxy substitution respectively were identified as significant inhibitors of inflammation when compared with the activity of standard drug Diclofenac. Conclusion: On comparing the docking scores of the compounds with their anti-inflammatory activity, it is evident that derivatives 6b, 6d and 6f that showed excellent docking scores, possessed maximum anti-inflammatory property.
 
Objective: We aimed to evaluate the use of ionic liquid in the synthesis of substituted Imidazo [1,2-a]pyridine derivatives and their antibacterial activity against Gram-positive and Gram-negative bacteria. Methods: The substituted-2-Phenylimidazo[1,2-a]pyridine derivatives have been Synthesized by a one pot two component reaction of 2-aminopyridine and α-halo acetophenone in the presence of green recoverable ionic liquid and ethanol. The newly synthesized compounds were characterized by elemental analysis, IR, 1H and 13C NMR. All the synthesized compounds were screened for their antibacterial activity. Results: Excellent yield of 2-Phenylimidazo[1,2-a]pyridine derivatives 3a-r were obtained in ionic liquid method than ethanol. The results of biologically activities show synthesized compounds would be of better use in drug development to combat bacterial infection in future. Conclusion: All the synthesized compounds were screened for antibacterial activity. Ampicillin, and cefixime were used as antibacterial references.
 
Histological section of mammary tissue of control and experimental rats  
Effect of TD and PGG on lipid peroxides in mammary gland of control and experimental animals. Values are expressed as mean±SD for six animals. Comparison is made as a-Group I vs Group II; b-Group II vs Groups III, IV and V; c-Group I vs Groups VI and VII. Statistical significance: *P<0.05. NS: Non significant Effect of TD and PGG on enzymic and non-enzymic antioxidants status The activities of enzymatic antioxidants, like SOD, CAT and GPx in the mammary tissue of control and experimental rats are represented in table 1. The status of these enzymes was significantly lowered in DMBA-induced (Group II) rats when compared to control (Group I) rats (p<0.05). On drug treatment (Group III and IV), the activities of these enzymes were found to be significantly (p<0.05) increased when compared with induced (Group II) rats. The drug  
p> Objective: To determine the effect of Tridham (TD) and 1,2,3,4,6-penta-O-galloyl-β-d-glucose(PGG) on lipid peroxidation levels and mitochondrial antioxidants status in experimental mammary carcinoma. Methods : Elaecoarpus ganitrus (fruits), Terminalia chebula (seed coats), Prosopis cineraria (leaves) , adult female albino rats of Sprague-Dawley strain weighing 170–190 g and 7,12-dimethylbenzeneanthracene (DMBA) were used for this study. Group I control rats, Group II rats mammary carcinoma induced with DMBA (25 mg in 1 ml olive oil) by gastric intubation. Group III, IV and V DMBA induced rats were treated with TD (400 mg/kg. b. wt/day), PGG (30 mg/kg. b. wt/day) and standard drug, Cyclophosphamide (30 mg/kg. b. wt/day), respectively for 48 d by gastric intubation. Group VI and VII rats served as TD and PGG treated controls, respectively for 48 d by gastric intubation. At the end of the experimental period, the rats were anaesthetized and sacrificed. Mammary glands were isolated and used for biochemical assays and histopathological evaluation. Results: In rats with cancer, the lipid peroxide levels (LPO) were significantly increased and mitochondrial antioxidant levels were decreased. Treatment with TD and PGG decreased LPO levels and increased mitochondrial antioxidant status in mammary carcinoma bearing rats. Histopathological analysis also confirmed the therapeutic effect of TD and PGG. No significant adverse effect was observed in sole drug treated group of rats. Conclusion: TD and PGG have definite therapeutic effect in experimental mammary carcinoma and inhibit growth of cancer cells by restoring mitochondrial antioxidant status and energy metabolism to normal states.</p
 
Multicomponent, solid-phase, microwave and grinding methods are the constructive modes in the sustainable synthesis of 1, 2, 4-triazoles and such reactions have attracted enormous interest in recent years. The alternative reaction conditions getting popularity in the recent ecofriendly-economical time have been thoroughly investigated. Literature studies on 1, 2, 4-triazoles have shown that these derivatives possess broad spectrum of biological activities. This review focuses on synthetic strategies and pharmacological properties of 1, 2, 4-triazoles.
 
The reaction of 5, 5'-(1, 4-phenylene)bis(4-amino-3-mercapto-4H-1,2,4-triazole) 1 with hydrazonoyl halides 2A,B gave a new series of 1,4-bis(6-substituted-7-(2-arylhydrazono)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-3-yl)benzene derivatives 4a-j. An alternate method to synthesize 4a-j was described. The structures of new compounds 4a-j were established on the basis of their elemental analysis and IR, 1H NMR, [13]C NMR and mass spectral data. All the title compounds were evaluated for their in vitro antimicrobial activity. All the compounds exhibited moderate to significant antibacterial and antifungal activities.
 
4-hydroxy benzhydrazide was converted to 4-amino-3-(4-hydroxy phenyl)-5-mercapto 1,2,4-triazole 1. This mercapto 1,2,4-triazole on condensation with substituted aromatic aldehyde in methanol with a trace of glacial acetic acid furnished mercaptobenzaldehyde hydrazones 2. This benzaldehyde hydrazones on condensation with thioglycollic acid in 1,4 -dioxane with pinch of ZnCl 2 furnished thiazolidinon 3. Similarly this mercapto 1,2,4-triazole on treatment with substituted aromatic carboxylic acid in POCl 3 underwent ring closer and furnished 1,3,4-triazoles 4. All the mercapto benzaldehyde hydrazones and 1,3,4-triazoles were screened for antibacterial activity.
 
Recently several pyrrolo triazine derivatives were identified as potentially active anticancer agents against vascular endothelial growth factor receptor (VEGFR) tyrosine kinases. 3D QSAR studies for the 10 molecules of various substituted pyrrolo[2,1-f][1,2,4] triazines by using k-Nearest Neighbor Molecular Field Analysis (kNN-MFA) combined with various selection procedures was performed. Using kNN-MFA approach 14 3D-QSAR models were generated; one of these models was selected on the basis of q2 and pred_r2 values. The selected model had shown good internal and external predictivity for the training set of 7 molecules and test set of 3 molecules with validation (q2) and cross validation (pred_r2) values of 0.9945 & 0.2096 respectively.
 
Overlay of close contacts of cis isomers: (pk 42 in magenta color and pk46 in green color) with neighboring amino acid residues 
Overlay of close contacts of trans isomers: (pk122) with neighboring amino acid residues 
Visualization of active binding sites of protein with bound ligand pk42 (oxazole) and 46 (triazole) 
Visualization of active binding sites of protein with bound ligand pk122 
p class="Default"> Objective: To identify the novel and simple bioactive antiandrogens, that can overcome to side effects as well as drug resistance. Methods: The AutoDock Vina (ADT) 1.5.6 software is used for molecular docking purposes. The molecular structures were drawn in ChemBiodraw ultra and by the help of ChemBiodraw 3D, all structures were energy minimized by MM2 method and converted to pdb extension file which is readable at the ADT interface. Results: Total ten compounds from both series were shown better binding affinity than R -bicalutamide including oxadiazole and triazole series. Among these pk42 and pk46 were studied in-depth which showed best binding affinity to the androgen receptor. The cis -isomers were found better than their trans -isomer. Conclusion: Novel 5-styryl-1,2,4-oxadiazole/triazole derivatives were studied through molecular modeling using Autodock Vina. The potent compounds which showed better binding affinity than R -bicalutamide like pk24 and 46 were further analyzed for their interactions. The conformational effect also found significant in binding to the androgen receptor.</p
 
Docked ligand molecule with secondary structure of the alpha-amylase with a nucleotide from salmonella typhi (PDB ID: 1B6O) in solid model  
Scheme 1: Synthesis of 2-[(E)-{[4-(1H-1,2,4-triazol-1-ylmethyl)phenyl]imino}methyl]phenol  
p> Objective: The main objectives of this research work is the synthesis and characterization of biologically potential triazole ring containing the Schiff base legend and their transition metal complexes, followed by screenings of their antimicrobial and anthelmintic activity the results of antimicrobial activity were compared with docking scores. Methods: The coordination complexes of Co(II), Cu(II), Fe(III) and Zn(II) with Schiff base derived ligand 4-(1 H -1,2,4-triazol-1-ylmethyl) aniline and substituted aldehydes have been synthesized. The complexes are characterized by elemental analysis, conductivity measurements, electronic, IR, and <sup>1</sup>H NMR spectral data. The synthesized compounds were also screened In vitro antimicrobial activity was carried out according to diffusion method by using agar and potato dextrose agar at 100, 500 and 700 mg/ml concentrations in DMF. HEX 8.0 programmers were used to perform the docking experiments on nucleotide of S. typhi at as ligand [PDB: 3B6O]. Results: Schiff base ligand and their transition metal complexes were studied for antimicrobial activity as well as docking. The results of both studies concluded that 4a, 4c and 4d compounds are more active in minimum inhibition concentration (30μg/ml) against Staphylococcus aureus ( S. aureus), Salmonella typhi (S. typlei) bacteria and Penicillium chrysogenum ( P. Crysogenum) fungi. The compounds showed highest docking score (-257.47,-275.61 and-280.17 respectively) with the secondary structure of the alpha-amylase with a nucleotide from s. typhi in the solid model. In the study of anthelmintic activity among these three compounds, 4d compound exhibits more activity compared with the standard. Conclusion: The compounds 4a, 4c and 4d were found to be more promising pharmacological activity this observation may promote a further development of this triazole group of compounds which may lead to better pharmacological profile than standard drugs. </p
 
Objective: The main objective of this work was to synthesize and evaluate the novel 2,3-dihydro-1,3,4-oxadiazole and 4,5-dihydro-1,2,4-triazole derivatives for cytotoxic activities. Methods: The 2,3-dihydro-1,3,4-oxadiazole derivatives 4a-h were synthesized by cyclization of N'-(substituted-benzylidene) isonicotinohydrazide 3a-e in refluxing acetic anhydride. The 2,3-dihydro-1,3,4-oxadiazole derivatives 4a-h were converted into the corresponding 4,5-dihydro-1,2,4-triazoles 5a-h using ammonia. All the synthesized compounds were identified, depending on the physical and spectral data. Title compounds were assessed for their cytotoxic activity against human cancer cell line (MCF-7) by using Sulforhodamine B (SRB) colorimetric assay. Results: All the synthesized compounds showed characteristic peaks in FTIR, 1HNMR and Mass spectral analysis. The results of the in vitro cytotoxic activity revealed that the compound 4c exhibited equipotent cytotoxic activity with an IC50 value of 8.04 µM when compared with that of standard drug doxorubicin (IC50= 8.02 µM). The reminder compounds have shown good to moderate cytotoxic activities when compared with that of a reference standard. Conclusion: We synthesized a series of title compounds in quantitative yields. Most derivatives showed moderate to good cytotoxic activity.
 
Derivatives of N-phenylbenzamide a 
Objective: N-phenylbenzamides are important and biologically active compounds. N-phenylbenzamides have been synthesized by some routes. An attempt has been made to find out the new route to synthesize N-phenylbenzamides. Methods: The reaction was carried out by reacting substituted benzoyl chlorides with 1,3-diphenylthiourea in the presence of triethylamine in THF at 70 °C. After 4hr the product was purified and identified. Results: An excellent and pure yield of N-phenylbenzamides was obtained by reacting substituted benzoyl chlorides with 1,3-diphenylthiourea. The proposed mechanism follows imino alcohol-amide tautomerism and suggests the involvement of rearrangement intermediate. Conclusion: 1,3-diphenylthiourea is inexpensive commodity chemical and it is found to be the useful reagent for the direct conversion to N-phenylbenzamide. The proposed mechanism follows imino alcohol-amide tautomerism and suggests the involvement of rearrangement intermediate. The synthesis gave pure, high yield, and the one and only isolated product.
 
A series of 5-substituted aryl / heteroaryl methylidene-1,3-thiazolidine-2,4-diones (1a-1j) were synthesised by knoevenagel condensation of 1,3- thiazolidene-2,4-dione with various aldehydes in toluene using piperidine as catalyst. Drug-likeness, protein binding energy calculation and docking simulations were carried out by in silico studies and the observed results suggest their possible hypoglycemic effect. Anti-oxidant potential of the series 1a-1j were examined by 2,2-diphenyl-1-picryl hydrazyl (DPPH) radical scavenging assay, superoxide anion radical scavenging assay and reducing power assay. Ascorbic acid and gallic acid are used as reference substances and their effects are compared with test compounds.
 
Objective: N-substituted derivatives of 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-4H-[1, 3] thiazeto [3, 2-a] quinoline-3-carboxylic acid: Synthesis and antibacterial activity. Methods: In the present study N-substituted derivatives of 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acid were prepared by using Triethylamine and DMF. This procedure was modified by adding tetra butyl ammonium bromide (TBAB) to facilitate completion in few reactions. Other reactions which did not proceed in both the aforementioned ways were facilitated by the use of Morwet-D425. All the new title compounds were characterized by their spectral data and were screened for antibacterial activity. Results: Some of the reported compounds were synthesized using the process disclosed by us in U.S.Pat.No.8, 410,268B2. In our present work, we have achieved good yields and purity. Many compounds exhibited substantial antibacterial activity. Conclusion: It can be inferred that the title compounds with substituted phenyl and quinoline rings exhibited comparable antibacterial activity with respect to the standard.
 
Object: To synthesise a series of 1-cyclopropyl-7-[4-(2,6-dimethyl-pyrimidin-2-yl-diazenyl)-piperzin-1-yl]-6-fluoro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid and 1-cyclopropyl-7-[4-(2,6 dimethoxy-pyrimidin-2-yl-diazenyl)-piperzin-1-yl]-6-fluoro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid and their dione derivatives and evaluate for their antibacterial activity. Method: A series of 1-cyclopropyl-7-[4-(2,6-dimethyl-pyrimidin-2-yl-diazenyl)-piperzin-1-yl]-6-fluoro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid and 1-cyclopropyl-7-[4-(2,6 dimethoxy-pyrimidin-2-yl-diazenyl)-piperzin-1-yl]-6-fluoro-4-oxo-1,4-dihydro-quinoline-3- carboxylic acid and their dione derivatives were synthesized in moderate yield and characterized by IR, 1H NMR spectra and elemental analysis. The compounds were evaluated for their in-vitro antibacterial activity against some Gram-positive and Gram-negative bacteria using conventional agar-dilution method. Result and Discussion: The antibacterial data's of the newly synthesized compounds indicate that some of them show better antibacterial activity than compared to their reference drug Ciprofloxacin. Conclusion: Ten (6a-j) new biologically active diketones were synthesized for the first time. Synthesized compounds exihibited good antibacterial activity against the tested bacteria.
 
ED50 of compounds 5, 13, and 19 in scPTZ screen
Ligands based design of series A 
Objective: Utilisation of the ligand-based design and molecular hybridization to design promising candidates with prospective efficacy and safety. Synthesis of the designed candidates using different synthetic methods. Biological evaluation of the newly synthesised candidates as anticonvulsant agents.Methods: Three novel series of 5-(benzo[d][1,3]dioxol-5-yl)-3-tert-butyl-4,5-dihydropyrazoles have been designed via ligand-based drug discovery and molecular hybridization. Proper synthetic routes have been followed in the preparation of compounds (2-23) which have been characterised by different spectral techniques. Antiepileptic potential was assessed by biological evaluation using ‘classical’ animal models of epilepsy, in addition to rotarod test for toxicity.Results: 4-Nitrophenyl derivatives (5, 13, and19) displayed the highest potency. Compound 5was the most active substituent in series A (N'-aroyl-3-tert-butyl-4,5-dihydro-1H-pyrazole-1-carbohydrazide). It was 2.7 and 1.3 times more active than reference drug Stiripentol (I) and lead compound III, respectively. Compound13 was the best candidate in series B (N'-arylidene-3-tert-butyl-4,5-dihydro-1H-pyrazole-1-carbohydrazide). It was 3.3, 1.5, and 1.2 times more potent than Stiripentol, lead compound III and new compound 5, respectively. Two members (19 and 21) of series C (1,3,4-oxadiazole derivatives) achieved 100 % protection at lower doses than I and III, being 2.6 and 2.4 times more active than Stiripentol. In scPTZ screen, the most active congeners (5, 13, 19) exhibited ED50 values of 45, 48, and 81 mg/kg, respectively, which are highly superior as compared to that of reference drug Stiripentol(I) and lead compound III (ED50 115 and 110 mg/kg, respectively).Conclusion: Ligand-based design together with molecular hybridization in drug design succeeded to produce potent and wide spectrum candidates.
 
Eight novel 2-amino-5-aryl-1,3,4-oxadiazole analogues were synthesized and screened for antibacterial and antifungal activity by liquid dilution method used for the determination of MIC (minimum inhibitory concentration). Structure of the synthesized compounds was confirmed by means of their IR, 1H-NMR, Mass spectroscopy and elemental analysis. Bacterial strains of Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus Subtilis and fungal strains of Aspergillus niger and Candida albicans were used in the study. Norfloxacin and clotrimazole was used as the standard positive control for antibacterial and antifungal activities respectively. MIC of the synthesized compounds ranged between 20-56 μg/mL and 42-78 μg/mL for antibacterial and antifungal activities respectively.
 
A novel series 7(a-f) 3-[5-(4-substituted) phenyl-1,3,4-oxadiazole-2yl]-2 phenylquinazoline-4(3H)-ones have been synthesized and screened for its percent growth inhibition on K 562 cell lines at different concentrations. IC 50 values of 7d, 7e and 7f have been reported. Doxorubicin was used as reference drug. Percent growth inhibition on K 562cell lines at 1 μM was found to be 50.1, 47.4 and 17.7 for compounds 7d, 7e and 7f. The results indicated that substitution of electronegative atoms showed low anticancer activity.
 
In present study 5,5'-(5-nitrobenzene-1,3-diyl)bis(1,3,4-oxadiazole-2-thiol)azo dye were synthesized by multistep reaction sequences, Structure of newly synthesized compounds characterized and confirmed by IR, NMR and Mass spectral studies. The synthesized compounds were screened for their antimicrobial and in vitro antioxidant properties. Synthesized compounds were found to be potent antibacterial and antioxidant agents. All the synthesized compounds exhibit significant biological activity and are certainly hold greater promise for discovering safer biologically active molecules.
 
In the present study, a series of S-substituted derivatives of 5-benzyl-1,3,4-oxadiazole-2-thiol were synthesized by converting phenyl acetic acid successively into ester, hydrazide and 1,3,4-oxadiazole. Finally the target compounds were obtained by stirring 5-benzyl-1,3,4-oxadiazole-2-thiol with different electrophiles in the presence of sodium hydride (NaH) and dimethyl formamide (DMF). The structure of synthesized compounds has been established by spectral data. All the compounds have been screened for their antimicrobial and hemolytic activity.
 
Objective: The objective of the present study is to synthesize Schiff base ligand, N,N' -bis(benzoin) 1,4 butane diimine and its Ni(II) and Zn(II) complexes. Methods: The synthesized complexes were characterized by IR and SEM. The synthesized Schiff base ligand and its Ni(II) and Zn(II) complexes were screened for antibacterial and antifungal activity. Results: IR data show that the complexes are four coordinate. The SEM show that all the complexes are nano crystalline. Conclusion: The synthesized complexes were tested against the bacterial and fungal species.The synthesized complexes were showed remarkable zone of inhibition with standards and have good antibacterial and antifungal activities.
 
Objective and methods: Reaction of cyanoacetohydrazide with different aromatic and heteroaromatic ketones yielded the corresponding hydrazones, which reacted with ketene dithioacetal in presence of KOH at room temperature to give pyridinedicarbonitrile derivatives. The latter compounds refluxed with hydrazine hydrate to give pyrazolo[4,3-c] pyridinecarbonitrile derivatives. Results: The structures of the newly synthesized compounds were confirmed by elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data. Nine compounds of the newly synthesized compounds were evaluated for their in-vitro anticancer activity against human breast cancer cell line (MCF-7). Conclusion: The results revealed that all such compounds exhibited lower activity in relation to the reference drug doxorubicin.
 
A series of N-aryl-2-(3-oxo-1, 4-benzothiazin-2-yl) acetamides have been synthesized by the condensation of different 3/4 substituted (3-nitro, 4-nitro, 3-methyl, 4-methyl, 3-chloro, 4-chloro) anilines with (2H)-oxo-3,3a-dihydrofuro [3,2-b][1,4-benzothiazine and screened for anticonvulsant activity. The condensation o-aminophenol with maleic anhydride yielded 2,3-dihydro-3-oxo (2H)-1,4-benzothiazin-2-yl-acetic acid which on reaction with thionyl chloride afforded (2H)-oxo-3,3a-dihydrofuro [3,2-b][1,4]-benzothiazine. The structures of the synthesized compounds have been established on the basis of elemental analysis and spectral data. All the synthesized compounds were subjected for anticonvulsant activity by using maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) methods. The synthesized compounds were administered intraperitoneally at the doses of 30, 100 and 300 mg/kg and were compared with the standard drugs i.e. phenytoin (MES group) and carbamazepine (scPTZ group). The abolition of hind limb tonic extensor spasm was recorded as a measure of anticonvulsant activity. All the compounds were found to possess anticonvulsant activity comparable to that of standard.
 
A new symmetrical Schiff base ligand was derived from 2-hydroxy-benzaldehyde, pyridine-2,6-diamine and benzene1,4-dicarbaldehyde and then it is allowed to react with metal salts to form binuclear Schiff base metal complexes. All the synthesized complexes were characterized based on elemental analyses, IR, 1H NMR, magnetic moment, molar conductance, ESR, UV, cyclic voltammetry and thermal analysis (TGA). The molar conductance data reveal that the chelates are electrolytes. An IR spectrum shows that the Schiff bases are coordinated to the metal ions in a manner with NNN donor sites of the pyridine ring, oxygen of phenolic OH group and NN donor sites of bipyridyl group. The formation of ligand was also ascertained by 1H NMR spectra. The electronic spectra and ESR measurements show that Cu(II), Co(II), Mn(II) and Ni(II) complexes has octahedral geometry. The cyclic voltammetric studies of these complexes in N,N-dimethylformamide indicate the structural changes during the course of redox reaction and quasi-reversible nature of the Schiff base binuclear complexes. Thermal stability of the complexes was also evaluated to assess the compatibility of the donating moieties. The synthesized ligands, in comparison to their metal complexes were screened for their antibacterial activity against bacterial species Staphylococcus aureus, Escherichia coli, Bacillus subtilis and Klebsilla pneumonia. The activity data show that the metal complexes are more potent antibacterial than the parent organic ligands against one or more bacterial species. DNA cleavage ability of the synthesized binuclear Schiff base metal complexes were also performed by gel electrophoresis.
 
One pot neat, solvent free green protocol of 1,5-benzothiazepines is reported here.1,3-substituted-prop-2-en-1-one 2a were synthesized by microwave -assisted Claisen-Schmidt condensation of acetylated α-naphthol with aldehydes in presence of alkali and ethanol. Synthesis of 2,3-dihydro-2-substituted-4-(naphthalen-2'-ol)-yl -1,5-benzothiazepines 3a was carried out by cyclo condensation of 1,3-substituted - prop-2-en-1-one 2a with 2-aminothiophenol in presence of ecofriendly catalyst zinc acetate in the solvent free condition under microwave irradiation. The structures of newly synthesized compounds were confirmed by spectral evidence and the compounds were evaluated for their anticonvulsant and CNS depressant activity. The compounds have shown excellent results.
 
A new series of 2,4-disubstituted-l,5-benzodiazepine derivatives were synthesized by the condensation of o-phenylendiamine and various 1-(4'- substituted phenyl)-3-(6″-methoxynapthaline)-2-propene-1-one under microwave irradiation. The structures of newly synthesized compounds were confirmed by IR, 1H NMR, mass and elemental analysis. All the compounds were tested for in vitro activities against a panel of Gram-positive and Gram-negative bacteria. All the compounds exhibited mild to moderate antimicrobial activity.
 
The cytotoxic effect of secondary metabolites extract of endophytic fungi (1.3.11, 1.1.6,.and 1.2.6) isolated from the fruit of "Tanaman Buah Makassar "on in-vitro T47D and MC-7 intact cells and identification of the fungus 1.3.11 by ITS regions of ribosomal DNA sequence were carried out. The cytotoxic effect of these extract (IC50) was assessed on T47D and MCF-7 cell (concentration 5-200 μg/ml) over 24 and 478 hr in CO2 using MTT methods on ELIZA reader at 595 nm. The results shows IC50 of fungi 1.3.11 and 1.2.6 were 7 and 50 μg/mL respectively. Extracts of fungi 1.1.6, however, showed weak or no cytotoxic effect toward T47D. Incubation of MCF-7 cells with extract of fungi 1.3.11, it showed an IC50 of 31 μg/mL. Furthermore, both T47D and MCF-7 cells showed pronounced morphological changes after 48 hour incubation with extracts of fungi 1.3.11 at 0.5 and 5 μg/mL. Moreover, T47D, but not MCF-7 cells showed morphological changes when incubated with extract of (i) fungi 1.2.6 (40 μg/mL) and (ii) fungi 1.1.6 (232 μg/mL). The results of identification of the fungus based on ribosomal DNA sequence show that it has highest DNA sequence similarity with Botryosphaeria parva.
 
Diameter of inhibition zone (mm) 
Objective: The main objective of this research were screened in vitro and in silico of 1,5-bis (3'-ethoxy-4'-hydroxyphenyl)-1,4-pentadiene-3-one as potential antibacterial agents.Methods: The in vitro antibacterial study was carried against Staphylococcus aureus, Staphylococcus epidermidis (gram positive) and Escherichia coli, Salmonella thypi (gram negative) using broth dilution method to determine Minimum Inhibitory Concentration (MIC), disc diffusion method to determine the diameter of inhibition zone. In silico antibacterial study was carried using computational software Protein-Ligand ANT System (PLANTS), computational docking was carried using receptor with Protein Data Bank (PDB) file 3MZD. The structures were optimized prior docking using YASARA, and MarvinSketch. The results of antibacterial testing were compared to two positive control drugs i. e amoxicillin and cefadroxil.Results: In vitro evaluation showed that 1,5-bis (3'-ethoxy-4'-hydroxyphenyl)-1,4-pentadiene-3-one has a better antibacterial activity than amoxicillin and cefadroxil with a Minimum Inhibitory Concentration (MIC) of 0.15 ppm and diameter of inhibition zone of 11.27±0.31, 11.35±0.39, 11.25±0.33, and 11.05±0.45 mm in Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, and Salmonella thypi, respectively. These results in line with in silico evaluation that showed 1,5-bis (3'-ethoxy-4'-hydroxyphenyl)-1,4-pentadiene-3-one has more negative docking score than amoxicillin, cefadroxil, and cloxacillin acyl as a native ligand on the 3MZD receptor.Conclusion: This results obtained in this research work were 1,5-bis (3'-ethoxy-4'-hydroxyphenyl)-1,4-pentadiene-3-one compound potential as an antibacterial agent.
 
Top-cited authors
Pemaiah Brindha
  • SASTRA University
Nirav Gheewala
  • Shree Dhanvantary Pharmacy College
Sanjay Patel
Natarajan Chandrasekaran
Vidyasagar Gunagambhire M
  • Gulbarga University