Bommineni Madhava Reddy

G. Pulla Reddy College of Pharmacy | GPRCP · Department of Pharmacy

Substituted triazoles have received considerable attention during the last two decades as they are endowed with a variety of biological activities and have a wide range of therapeutic properties. The present work is concerned with the synthesis of fused 1, 2, 4-triazole derivatives with the objective of discovering novel and potent anti-tubercular...

The different extracts of the roots of Helicteres isora (Family-Sterculiaceae) were tested for anti-diabetic activity, by glucose tolerance test in normal rats and alloxan induced diabetic rats. Aqueous ethanol and butanol extracts had shown significant protection and lowered the blood glucose levels to normal in glucose tolerance test. In alloxan...

The different extracts of the roots of Helicteres isora (Family-Sterculiaceae) were tested for anti-diabetic activity, by glucose tolerance test in normal rats and alloxan induced diabetic rats. Aqueous ethanol and butanol extracts had shown significant protection and lowered the blood glucose levels to normal in glucose tolerance test. In alloxan...

Aim: To synthesize novel pyrano quinolines by one-pot multicomponent reaction under noncatalytic conditions, further it was proposed to investigate the reactivity of pyrano quinolines with the oxidizing agent like iodobenzene diacetate (IBD). Synthesized compounds were evaluated for antibacterial activity. Materials and Methods: Synthetic procedure...

Condensation of 2-methyl-4H-1,3-benzoxazine-4-one (1) with p-amino acetophenone gave 3-(4-acetylphenyl)-2-methylquinazolin-4(3H)-one(2). Claisen-Schmidt condensation of compound 2 with different aromatic and heterocyclic aldehydes afforded different quinazolyl chalcones 3(a-h) which on refluxing with hydroxylamine hydrochloride gave 3-(4-(5-(3-subs...

Cyclization of 1-azido-4-methoxy benzene (1) with acetyl acetone in presence of sodium ethoxide gave 1-(4-methoxyphenyl)-5-methyl-1H-1,2,3-triazole-4-yl)ethanone(2). Claisen-Schmidt condensation of compound 2 with different aromatic and heretocyclic aldehydes afforded triazolyl Chalcones (3a-h) which on refluxing with hydroxylamine hydrochloride in...

Six new derivatives of pyrazoline incorporated imidazo(1,2-a)pyridines 6(a-f) were synthesized and evaluated against anti inflammatory and invitro anti cancer activities. Claisen-Schmidt condensation of 2-aryl imidazo(1,2-a) carbaldehydes (4a & 4b) with substituted acetophenones gave 2-aryl imidazo pyridinyl chalcones 5(a-f). Cyclization of 5(a-f)...

Codensation of different phenacyl bromides with 2-amino pyridine afforded 2-aryl imidazo(1,2-a) pyridines 1(a-e). Vilsmeier-Haack reaction of 1(a-e) gave 2-aryl imidazo (1,2-a) pyridine-3-carbaldehydes 2(a-e). Further, the condensation of these carbaldehydes with thiazolidinedione in glacial acetic acid gave (5-[2-aryl imidazo [1,2-a]pyridine-3-yl]...

Synthesis, cytotoxic and anti-microbial screening of novel thiobarbituric acid incorporated pyrazole derivatives were performed. Vilsmeier-Haack reaction of different phenyl hydrazones 1(a-e) afforded pyrazole -4- carbaldehydes 2(a-e) in good yields. Knoevenagel condensation of compounds 2(a-e) with thiobarbituric acid gave a series of 5-ylidene de...

New derivatives of isatin conjugated 4-azidopyrazolines were synthesized 5(a-e) and characterized by physical and spectral data. From p-aminoacetophenone, 1-(4-azidophenyl)ethanone (1) was prepared by diazotization and subsequent reaction with sodium az ide. Claisen-Schmidt condensation of compound (1) with different aromatic/hetero aldehydes gave...

Cyclization of 1-azido-4-methoxy benzene (1) with acetyl acetone in presence of sodium ethoxide gave 1-(4-methoxyphenyl)-5-methyl-1H-1,2,3-triazole-4-yl) ethanone (2). Claisen-Schmidt condensation of compound (2) with different aromatic and heretocyclic aldehydes afforded triazolyl chalcones (3a-h) which on refluxing with hydroxylamine hydrochlorid...

Suppositories are the convenient way of administering drugs in infants. In view of the lack of suitable pediatric antiretroviral formulations in the market, suppositories containing fixed dose combination (FDC) of stavudine, lamivudine and nevirapine (SLN) were developed to allow administration of the correct weight-related dose in pediatric HIV pa...

Objective: Ethnobotanical survey of Schrebera swietenioides Roxb revealed the bark of the tree to be useful in anemia. The objective of this study was to study the ant-anemic effect of methanolic extract of root bark of S. swietenioides Roxb. against phenylhydrazine induced anemic rat model. Methods: The methanolic extracts of Leaf, Stem bark, and...

A simple, accurate isocratic reverse phase high performance liquid chromatography (RP-HPLC) method was developed for the determination of the plasma concentration of naringin, a flavanone glycoside in rat plasma. An assay procedure involved simple liquid-liquid extraction of naringin from plasma directly into methanol. The organic layer was separat...

A new series of 1H-pyridin-4-yl-indazole-3-carboxylic acid and its derivatives were synthesized from indazole-3-carboxylic acid methyl ester and 2-cyano-4-chloropyridine. All the new compounds have been characterized by spectral data and subsequently evaluated for their anti-inflammatory and analgesic activity. Graphical Abstract A new series of 1H...

Plants represent a major potential source of drugs for treating diabetes. The study of plants having antidiabetic activity may give a new approach in the treatment of diabetes mellitus. Tragia plukenetii is traditionally claimed to be useful in the treatment of diabetes. The present study was intended to evaluate the antihyperglycemic activity of a...

New series of isoniazid incorporated 2-styrylquinazolinone derivatives were synthesized by condensing 2-methyl-4H-3,1-benzoxazin-4-one with isoniazid and subsequent reaction with different aryl/heterocyclic aldehydes. The structures of newly synthesized compounds were confirmed on the basis of physical and spectral data. In anti-tubercular screenin...

Objective: To synthesize pyrazolyl thiazolidinediones i.e., 2, 4-thiazolidinedione incorporated pyrazole derivatives anticipating effective anti-cancerdrugs. Methods: Different substituted pyrazole carbaldehydes which were synthesized by Vilsmeier-Haack reaction of substituted phenyl hydrazones with POCl3 and dimethyl formamide, hybridized with 2,...

Cyclisation of 1-(2-hydroxyphenyl)-3-substituted phenylprop-2-en-1-ones 1a-h in pyridine with mercuric acetate gives different 2-benzylidene-1- benzofuran-3(2H)-ones 2a-h which on subsequent reaction with hydroxylamine hydrochloride affords 2-benzylidene-1-benzofuran-3(2H)-one oximes 3a-h. These oximes on reaction with benzoyl chloride / p-toluene...

A series of novel pyrazolyl tetrazoles were synthesized by introducing tetrazole moiety at the fourth position of 1,3-substituted pyrazole nucleus. Synthesis was carried out by cyclization of different pyrazolonitriles using sodium azide in the presence of triethylammonium chloride as phase transfer catalyst. The structures of the synthesized compo...

A series of new 2,5-disubstituted-1,3,4-oxadiazole derivatives 8(a-o) was synthesized by the reaction of 1-(5-phenyl-1,3,4-oxadiazol-2-yl)piperazine with various sulfonyl chlorides. The synthesized compounds were characterized by elemental analyses, 1H NMR, 13C NMR and mass spectral studies. The newly synthesized compounds were screened for their a...

A series of 5-(alkyl(1H-indol-3-yl))-2-(substituted)-1,3,4-oxadiazoles were efficiently synthesized by oxidative cyclisation of N'-benzylidene-(1H-indol-3-yl)alkane hydrazides using di(acetoxy)iodobenzene. N'-Benzylidene-(1H-indol-3-yl)alkane hydrazides themselves were derived from simple indole-3-carboxylic acids. The 5-(alkyl(1H-indol-3-yl))-2-(s...

Ethnopharmacological relevance: The bark of Tecomella undulata is traditionally claimed in the treatment of various disease ailments including obesity and cancer. Till now there are no studies about anti-obesity activity of Tecomella undulata bark. Aim of the study: The present study was aimed to establish a scientific evidence for anti-obesity...

Export Date: 18 October 2014

Antioxidant activity of ethanolic extract of Caralluma attenuata was evaluated for its free radical scavenging property in different in vitro models. The extract showed good dose dependent free radical scavenging property in all models except in inhibition of nitric oxide radical and lipid peroxidation. IC50 values are found to be 10, 14, 110 μg/mL...

Pupalia lappacea Juss (Family: Amaranthaceae) is claimed to be useful in treatment of bone fracture, wounds, boils, cough, toothache, fever and malaria. The study was aimed to evaluate the 80% aqueous ethanolic extract of aerial parts of P. lappacea for antinociceptive and antipyretic activities to verify the traditional claim. The extract was oral...

Quinoxaline-incorporated Schiff bases (4a–j) were synthesized by the condensation of 2-[(3-methylquinoxalin-2-yl)oxy]acetohydrazide (3) with indole-3-carbaldehyde, furfuraldehyde, 5-(4-nitrophenyl)-2-furfuraldehyde, and substituted benzaldehydes under conventional and microwave irradiation methods. The microwave method was found to be remarkably su...

Cancer is one of the most prominent human diseases which has enthused scientific and commercial interest in the discovery of newer anticancer agents from natural sources. Here we demonstrated the anticancer activity of ethanolic extract of aerial parts of Pupalia lappacea (L) Juss (Amaranthaceae) (EAPL) on Chronic Myeloid Leukemia K562 cells. Antip...

Figure S1A: HPLC chromatogram of standard Rutin (15, 25, 50, 75 and 100 ppm) and sample (EAPL). Figure S1B: HPLC chromatogram of ethanolic extract of aerial parts of Pupalia lappacea. (DOC 66 kb)

Croton caudatus (Euphorbiaceae) is claimed to be useful in treatment of sprains, arthritis and liver disorders in traditional system of medicine. In the present investigation antinociceptive, anti-inflammatory and antipyretic effects of the 80% aqueous ethanolic extract from leaves of C. caudatus have been evaluated. The ethanolic extract reduced t...

The aqueous ethanolic extract of Pandanus odoratissimus (Pandanaceae) root was tested for its effect on blood glucose levels in normal and diabetic rats. Hypoglycemia was observed in basal conditions when tested at an oral dose of 75,150 and 300 mg/kg body weight. The ethanolic extract has displayed a significant dose-dependent antihyperglycemic ac...

Starch isolated from Trapa bispinosa (Trapaceae) fruit was studied as an alternative pharmaceutical excipient to maize starch. T. bispinosa starch has been evaluated by series of tests as mentioned in Indian Pharmacopoeia before being used for evaluation. It was tested along with maize starch as an alternative excipient by performing battery of pre...

Piperine (CAS no: 94-62-2), an alkaloid obtained from Piper nigrum and P. longum is a known inhibitor of various enzymes (CYP isozymes) responsible for biotransformation of drugs. By inhibiting the metabolism of drugs, piperine improves the bioavailability of drugs. In the present study piperine (10 mg/kg) significantly increased the dose-dependent...

An ecofriendly green approach for synthesis of substituted pyrano[2,3-c]pyrazoles has been developed via a multicomponent one pot approach in aqueous ethanol medium under totally non-catalytic conditions. The synthesized compounds were evaluated for their antibacterial, anti-inflammatory and cytotoxic activities.

Novel benzimidazole derivatives possessing two different structural moieties (III) and (VII) are synthesized.

Quinoxaline incorporated Schiff bases (4a-j) were synthesized by the condensation of 2-[(3-methylquinoxalin-2-yl)oxy] acetohydrazide (3) with indole-3-carbaldehyde, furfuraldehyde, 5-(4-nitrophenyl)-2-furfuraldehyde and substituted benzaldehydes under conventional and microwave irradiation methods. The microwave method was found to be remarkably su...

Vilsmeier-Haack reaction of substituted phenyl hydrazone derivatives (1a-j) afforded 1,3-substituted diphenyl-1H-pyrazole-4-carbaldehydes (2a-j). Compounds (2a-j) on condensation with malonic acid gave (2E)-3-(1,3-substituted diphenyl-1H-pyrazol-4-yl) acrylic acids (3a-j) which on reaction with thionyl chloride afforded acryloyl chlorides. The reac...

Pyrazole-1H-4-yl-acrylic acids (3a-j) were prepared from pyrazole-1H-4-carbaldehydes which in turn were prepared by the Vilsmeier-Haack reaction of phenyl hydrazone derivatives (1a-j). The reaction of pyrazole-1H-4-yl-acrylic acids to 3-(1, 3-diphenyl-1H-pyrazol-4-yl) propanoic acids (4a-j) was carried out using Pd-charcoal and diimide methods and...

Ethyl acetate and methanol extracts of the Carallia brachiata bark were tested for hepatoprotective activity against carbon tetrachloride (CCl 4) induced hepatotoxicity in rats at dose levels of 250 and 400 mg/kg body weight. The ethyl acetate extract has shown high significance by lowering the biochemical parameters such as serum glutamate pyruvat...

Piperine (CAS 94-62-2), an alkaloid obtained from Piper nigrum and P. longum, is a known inhibitor of various enzymes (CYP isozymes) responsible for biotransformation of drugs. By inhibiting the metabolism of drugs, piperine improves the bioavailability of drugs. In the present study piperine (10 mg/kg) significantly increased the dose-dependent an...

Starch isolated from Caralluma attenuata plant was studied as an alternative pharmaceutical excipient to maize and potato starch. The C. attenuata starch has been evaluated by series of tests as mentioned in Indian Pharmacopoeia before being used for evaluation. It was tested along with maize and potato starch as an alternative excipient by perform...

1,3-Dipolar cycloaddition of nitrile oxide generated from substituted pyridinyloxy benzaldoximes with styrene or α,β-unsaturated ketones produces a series of 3,5-disubstituted-4,5-dihydroisoxazoles and 3,4,5-trisubstituted isoxazoles. On the other hand, C-chlorooxime reacts with α,β-unsaturated ketones yielding 3,4,5-trisubstituted isoxazoles. All...

In view of the lack of suitable paediatric antiretroviral formulations in the market, a fixed dose combination (FDC) dispersible tablet containing Stavudine, Lamivudine and Nevirapine was developed to allow administration of the correct weight-related dose in paediatric HIV patients as recommended by WHO. Dispersible tablets were prepared by direct...

Strobilanthes meeboldii (Acanthaceae) is an ornamental plant and is claimed to be useful in treatment of pains in traditional system of medicine. In the present work, the antinociceptive and central nervous system (CNS) depressant effects of the 80% aqueous ethanolic extract from aerial parts of S. meeboldii have been evaluated. The ethanolic extra...

Vilsmeier-Haack reaction of phenyl hydrazone derivatives (1a-j) afforded 1,3-diphenyl-1 W-pyrazole-4-carbaldehydes (2a-j). Condensation of (2a-j) with malonic acid gave 3-(1,3-diphenyl-1/-/-pyrazol-4-yl) acrylic acids (3a-j. Reduction of (3a-j) gave 3-(1,3-diphenyl-1H-pyrazol-4-yl) propanoic acids (4a-j). The structures of the newly synthesized com...

A series of pyrazolines (2a-j) have been synthesized and evaluated for their antimicrobial and antiinflammatory activities. The structures of the synthesized compounds have been confirmed on the basis of physical and spectral data. Compounds 2b, 2c, 2e and 2g have shown moderate antibacterial activity. None of the synthesized compounds showed antif...

A simple, inexpensive and rapid, stability indicating isocratic HPLC method has been developed for the quantitative determination of rimonabant, an anti-obesity drug. Degradation studies were performed on the bulk drug by heating to 105°C, exposure to UV light at 254 nm, acid (0.1 N hydrochloric acid), base (0.1 N sodium hydroxide) and aqueous hydr...

A simple, precise and rapid RP-HPLC method was developed for the determination of rimonabant in bulk as well as in formulations. The quantitation was carried out using Ace-C18, 150 x 4.0 mm column in isocratic mode, with mobile phase consisting of acetate buffer and acetonitrile in the ratio 30:70. The detection wavelength was 250 nm and the flow r...

Caralluma attenuata is traditionally claimed to be useful in the treatment of migraine. In the present study, various organic extracts of C. attenuata were investigated for their antinociceptive activity. Male Swiss Albino mice were used to test the antinociceptive activity on acetic acid-induced writhing and hot plate test, at an oral dose of 250...

The antihyperglycemic and hypolipidemic activities of Helicteres isora Linn. (Sterculiaceae) root extracts were investigated in alloxan-induced diabetic rats and a possible mechanism of the blood glucose lowering action was studied. Alloxan-induced diabetic rats experienced 69.13 and 51.14%, 22.60 and 21.89%, 30.12 and 19.96%, and 50.05 and 34.29%...

The stem bark of Carallia brachiata was studied for wound healing activity. The bark was extracted with petroleum ether, ethyl acetate and methanol successively. All the extracts were screened for wound healing activity by excision and incision models in Wistar rats. The ethyl acetate and methanol extracts were found to possess significant wound he...

Cynodon dactylon pers (fam. Poaceae) whole plant is used in traditional system of medicine for the treatment of diarrhea. In the present investigation hexane, dichloromethane, ethyl acetate and methanol extracts of Cynodon dactylon whole plant were tested for anti diarrheal activity on castor oil induced diarrhea, gastro intestinal motility by char...

A new series of 7-methoxy-4-methyl-8- [5-(aryl) isoxazol-3-yl]-2H- benzopyran-2-ones (6a-i) were synthesized by cyclization of chalcones, 8-(2-substituted prop-2-ene)-7- methoxy-4-methyl-2H-benzopyran-2-ones (5a-i) with hydroxylamine hydrochloride. The structures of the synthesized compounds have been established on the basis of physical and spectr...

The effect of administrating different extracts of Helicteres isora L. (Sterculiaceae) roots on blood glucose levels in normal and alloxan-induced diabetic rats was evaluated in this study. Among the five fractions (aqueous ethanol, chloroform, ethyl acetate, butanol and left over aqueous), the butanol fraction at a dose of 250 mg/kg showed maximum...

Abstract Arjungenin and arjunglucoside-I have been isolated and characterised from an alcohol extract of the fruits of Terminalia chebula Retz. (Combretaceae); their 13C NMR data are reported for the first time.

The various organic extracts of Helicteres isora Linn (Sterculiaceae) root were tested for anti-inflammatory activity using carrageenan-induced paw edema and for analgesic effect using hot plate test. The chloroform extract of Helicteres isora administered orally at doses of 250 mg/kg had a significant anti-inflammatory activity with 35.48% reducti...

Helicteres isora root extracts were studied for antinociceptive activity on acetic acid-induced writhing test in mice, at a dose of 250 mg/kg. Petroleum ether, chloroform and aqueous ethanol extracts have shown significant activity.

The antipyretic effect of the hexane, chloroform, ethyl acetate and methanol extracts obtained from Rumex nepalensis (Polygonaceae) roots was investigated in rats at 500 mg/kg by oral route. The investigation results showed that hexane and methanol extracts have significant antipyretic activity. The results provide a scientific rationale for the fo...

The ethanol, ethyl acetate and butanol extracts of Helicteres isora root showed significant oral hypoglycemic activity on glucose loaded rats at a dose of 250 mg/kg. The butanol extract showed maximum antihyperglycemic activity and effect being comparable to that of glibenclamide.

Pharmacognostic studies on the shape, microscopic structure, and morphology of Rumex nepalensis (Polygonaceae) were carried out. These studies provided referential information for identification of this crude drug.

A simple and sensitive spectrophotometric method in ultraviolet region has been developed for the determination of phyllanthin in different parts of Phyllanthus niruri. Phyllanthin shows maximum absorbance at 280 nm. Beer's law is obeyed in the concentration range of 5-50 μg/ml. The proposed method is precise, accurate and reproducible.

Extracts of Caralluma attenuata are screened for their antihyperglycemic activity. Ethanol, chloroform and butanol extracts were tested on glucose loaded and alloxan-induced diabetic rats. In both tests, the butanol extract, at the oral dose of 250 mg/kg, has shown statistically significant and considerable antihyperglycemic activity.

The phytochemical study using Caralluma umbellata (Asclepiadaceae) whole plant allowed the isolation of a novel pregnane glycoside named carumbelloside-I (3-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl-3beta,14beta -dihydroxypregn-5-en-20-one). Carumbelloside-I was evaluated for both antinociceptive activity and anti-inflammatory activity....

Various organic extracts of Sida rhomboidea leaves were studied for antinociceptive and anti-inflammatory activity at a dose of 200 mg/kg. Ethyl acetate extract has shown significant (P < 0.01) antinociceptive activity. Percentage inhibition of edema by butanolic extract (33.05, P < 0.001) is comparable to that of phenylbutazone, 100 mg/kg inhibiti...

Luteolin-4'-O-neohesperidoside, i.e. luteolin-4'-O-[alpha-(L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranoside)] has significant anti-inflammatory action. It is more potent than ibuprofen. Its antinociceptive activity is less pronounced when compared with its anti-inflammatory activity.

From the whole plant of Caraluma umbellata, three new C-21 steroidal glycosides, named as carumbellosides III-V, were isolated and their structures elucidated by extensive spectroscopic experiments, devoid of any derivatisation, as caralumagenin 3-O-beta-D-glucopyranosyl(1-->4)-beta-D-digitalopyranoside-20-O-be ta- D-glucopyranoside, caralumagenin...

Two plants, S. nobilis and C. stalagmifera, were studied for anti-inflammatory activity. The aqueous and butanol extracts of the two fresh whole plants were tested on carrageenan-induced rat paw oedema and kaolin-induced arthritis in rats. Both plants have shown significant anti-inflammatory and antiarthritic activities.

From the seeds of Semecarpus anacardium, a new phenolic glucoside, anacardoside, was isolated, and its structure and configuration were elucidated by a combination of NMR techniques as 1-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyloxy-3-hydro xy-5-methylbenzene.

From Caralluma umbellata, two new pregnane glycosides, named carumbelloside I and II, were isolated and their structures and stereochemistry were elucidated by a combination of NMR techniques as 3-O-β-d-glucopyranosyl-(1→6)-β-d-glucopyranosyl-3β,14β-dihydroxypregn-5-en-20-one and 3-O-β-d-glucopyranosyl-3β,14β-dihydroxypregn-5-en-20-one. The ambiguo...

The use of rifampin and clofazimine ointments alone and in combination over the patches of tuberculoid patients had a beneficial effect. In combination (rifampin and clofazimine), erythema, inflammation, and edema are considerably reduced. For some of the cases with a recent appearance of a patch, the patch completely disappeared. It is suggested t...

The different extracts of the roots of Helicteres isora (Family-Sterculiaceae) were tested for anti-diabetic activity, by glucose tolerance test in normal rats and alloxan induced diabetic rats. Aqueous ethanol and butanol extracts had shown significant protection and lowered the blood glucose levels to normal in glucose tolerance test. In alloxan...