Density (ρ), and Ultrasonic velocity (U) in binary mixtures of thiazolyl substituted schiff's bases with dioxane-water, acetone-water and ethanol-water mixture were measured at 30°C by using a Ultrasonic Interferometer at a frequency of 1 MHz. The study was carried out with change in concentrations & were used to calculate various thermodynamic parameters such as adiabatic compressibility (βs), Apparent molar compressibility (φ1K) Apparent molar volume (φ1V), intermolecular free length (Lf), specific acoustic impedance (Z) and relative association (RA).The results were used to discussed the interaction between solute and solvent.
The interaction of lanthanide metal ions with substituted heterocyclic drug has been investigated in 30% dioxane-water mixture at 0.1M ionic strength and 303K by Potentiometric titration. The data obtained is used to estimate the values of proton-ligand stability constant (pK) and metal-ligand stability constant (logK). It is observed that lanthanide ions forms 1:1 and 1:2 complexes with substituted heterocyclic drug.
The dense structure required by mixed-ionic and electronic conducting (MIEC) membrane based on La 0.6 Sr 0.4 Co 0.2 Fe 0.8 O 3-δ (LSCF) material could be influenced by the particle size of the LSCF, as this densification involves sintering of the particles. The particle size could be determined by using an appropriate synthesis method. The aim of this work is to investigate the effect of synthesis method to the particle size of the resulted powders. In this work, LSCF was successfully synthesized by sol-gel, co-precipitation, and solid-state methods. The coprecipitation is carried out with and without aging treatment after addition of precipitating agent. All LSCFs have a structure similar to the LaCoO3 structure as mother compound. Solid-state and co-precipitation with aging treatment can produce LSCF with high purity. Meanwhile, there were still other phases in LSCFs which were synthesized by sol-gel and co-precipitation methods without aging treatment. Other phases that appear are estimated from the Co 3 O 4 for co-precipitation method without aging treatment and Co 3 O 4 and Fe 2 O 3 for sol-gel method. The solid-state method is capable of producing particles with the highest crystallinity compared to other methods. The TGA results from LSCF with the sol-gel method and co-precipitation (without and with aging time) showed that the perovskite could be formed at temperature 650 °C. Characterization of LSCF particles with Scanning Electron Microscope (SEM) showed that all samples had irregular particle shapes, with uniformly small particle for sol-gel method, and the possibility of formation of large particle for co-precipitation method. However, Particle Size Analysis (PSA) analysis shows that in general, the co-precipitation method could produce smaller particle (particle size 1904.1 nm) than the solid-state method (particle size 2812.4 nm).
La0.7Sr0.3FexMn1-xO3 for (x=0.20 and 0.30) compound was modified by substituting Fe at Mn site in order to study different physical properties for its use as the cathode of SOFCs. The solid-state method was used to synthesize the material. The single crystallized phase was observed by X-ray diffraction and the size of the particle was observed to be in micrometer. Micrographs obtained from scanning electron microscope indicate a decrease in grain size with Fe doping. Density was calculated by Archimedes Principle and calculated values indicate increases in density with Fe substitution. Thermal expansion coefficient (TEC) observed by dilatometer decreased with Fe doping and thermogravimetric analysis showed weight gain by the compound with the rise in temperature. Impedance spectroscope recognized the non-Debye relaxation behavior of the compounds. Fe- substitution enhanced the conductivity and decreased the activation energy. Investigated parameters indicated that the prepared perovskite compounds are suitable for cathode application in SOFC.
This paper studies C6H18N4 (Triethylenetetramine; TETA) corrosion-resistance behavior on reinforcing-steel in concreteimmersed in 0.5 M H2SO4. Analyses showed that the corrosion inhibition efficiency increases as theconcentration of C6H18N4 admixture increases, whereby the inhibition efficiency also portrayed excellent correlation model (at r = 98.82%, Nash Sutcliffe Efficiency (NSE) = 97.65%, Analysis of Variance (ANOVA) p-value = 0.0350) with function of the C6H18N4 concentration admixed in the concrete. The optimal resistance to reinforcing-steel corrosion, in the study, was exhibited in the concrete sample having 0.1824 M C6H18N4 admixture, from which inhibition efficiency η = 94.78% was attained. The results support the suitability of C6H18N4 for inhibiting reinforcing-steel corrosion in concrete for the industrial/microbial medium, simulated by the 0.5 M H2SO4.
In the present methodology, we have reported the synthesis of substituted phenyl quinoxaline derivatives by using 1,2-phenylenediamines and α- tosyl ketones in presence of L-Proline as a catalyst and dichloromethane as solvent. This methodology is useful for the synthesis of quinoxaline derivatives with high yields.
A series of some novel 5-(5-substitutedphenyl)-4H-l,2,4-triazole-3-yl-1,3- benzoxazoles 3a-o were synthesized from 2-substituted-5-carbomethoxy benzoxazole 1. 2-substituted-5-carbomethoxy benzoxazoles on reaction with hydrazine hydrate resulted in the formation of 2-substituted 1,3-benzoxazole-5-carbonhydrazides 2a-c. The subsequent treatment of compounds 2 with an appropriate aromatic aldehyde in presence of ammonium acetate leads to the synthesis of die target compounds in good yields. The chemical structures of the newly synthesized compounds were elucidated by dieir IR, 1H NMR, 13C NMR and Mass spectral data analysis.
1,4,5-trisubstituted 1,2,3-triazoles were prepared by 1,3-dipolar cycloaddition reaction of some 2-substituted phenyl azides to dimethylacetylene dicarboxylate (DMAD) under regular stirring at room temperature or under microwave irradiation. The targeted compounds were obtained in good to excellent yields. The use of microwave irradiation gives the highest yields in few minutes and proper products.
The final targets are established by different types of functional groups on aryl azides with terminal alkynes of pefloxacin via click chemistry in conventional and microwave irradiation conditions. A series of novel derivatives are characterized by proton, carbon nuclear magnetic resonance technique and mass spectral techniques. From screening antibacterial results the 5c, 5d, 5e, 5f and 5g exhibited outstanding activity against Gram-positive and Gram-negative microorganisms compared to CPF. All the title compounds were subjected to molecular docking prediction and compounds 5h, 5a, 5g possesses the highest binding energy ΔG= –8.12, –7.61, –7.26 Kcal/mol, hydrogen bonding amino acid interactions Val40, Asp83, Lys93, Tyr23, Arg28 with the active site of Topoisomerase-IV from S. pneumoniae (4KPE). Further investigation, these compounds were evaluated to their molecular properties prediction by Molinspiration and Molsoft
Herein, we depict the reaction subbed with a blending bar originate the alkyne (III) and azide was added CuSO4/sodium ascorbate of 1.2 eq K2CO3 and the response combination was mixed at RT for 16-18 h. After work up to bear the preferred 1-((1-aryl) - 1H-1,2,3-triazol-4-yl) methyl) quinoxalin-2(1H)- ones (IV a-IV j) item. This large number of mixtures were evaluated for their hostile to disease action against human malignant growth cell lines by means of MCF-7,A-549 and HeLa. In vitro against malignant growth movement uncovers that a couple of mixtures displayed strong inhibitory in an assortment of disease cell lines. Among them 1-((1-(2,4- dimethoxyphenyl)- 1H-1,2,3-triazol-4-yl)methyl)pyrido[2,3-b]pyrazin-2(1H)- one (IV j) with 2,4-OCH3C6H3 MCF7 (3.64 ± 0.92), HeLa (4.62 ± 0.29), A-549 (8.02 ± 0.94) promising enemy of multiply movement .1-((1-(4- nitrophenyl)- 1H-1,2,3-triazol-4-yl)methyl)pyrido[2,3-b]pyrazin-2(1H)- one(IVi) with p-NO2C6H4 MCF-7 (4.15 ± 1.02), HeLa (6.43 ± 1.67), A-549 (10.74 ± 1.88) potent.1-((1-(2,4-dichlorophenyl)- 1H-1,2,3-triazol-4- yl)methyl)pyrido[2,3-b]pyrazin-2(1H)- one (IV h) with 2,4-ClC6H3 MCF-7 (5.02 ± 1.38), HeLa (8.84 ± 2.01), A-549 (12.18 ± 2.82) great action. Etoposide utilized as a positive control.
Here we described the synthesis of novel 1,2,3-triazole linked thiazolidine-2,4-dione and carbazole derivatives and
screened for their anticancer activities against three human cancer cell lines, MCF-7, HeLa and SKOV3 using MTT
assay. The newly synthesized triazole hybrids are characterized using 1H NMR, 13C NMR, IR and Mass spectral
data. The results indicated that the most potent compound in this series is compound 3b against MCF-7, compound
3i against HeLa and compound 3d against SKOV3, which showed the highest activity with IC50 value of 32.92
µg/ml, 12.08 µg/ml and 29.06 µg/ml respectively.
Keywords: 1,2,3-triazole, Carbazole, Thiazolidine-2,4-dione, Anticancer Activity
The active pharmaceutical ingredient, 2-Cyclohexylcarbonyl-4-oxo-1,2,3,6,7,11 b-hexahydro-4H-pyrazino[2,1-a] isoquinoline has been achieved in a deep eutectic solvent (DES) which is an efficient, green and novel route of synthesis. The synthesis involves three N-alkylation/acylation reactions. The corresponding reactions using inexpensive raw materials proceed efficiently in a deep eutectic solvent (DES) with an improved yield that makes synthesis cost effective. The present reaction offers excellent selectivity which lacks a product of N, N-dialkylation. Ease of recovery and reusability of DES makes this process efficient and environment-friendly.
A series of novel 3-alkyl(aryl)-4-(3-hydroxy-4-methoxybenzylidenamino)-4,5-dihydro-1H-1,2,4-triazol-5-ones (3a-j) were synthesized from the reactions of 3-alkyl(aryl)-4-amino-4,5-dihydro-1H-1,2,4-triazol-5-ones (2a-j) with 3-hydroxy-4-methoxy-benzaldehyde (3). The new ten compounds were characterized using by IR, 1H-NMR, 13C-NMR and UV spectral data. In addition, the synthesized compounds were analyzed for their in vitro potential antioxidant activities in three different methods. Compounds 3f and 3h showed best activity for the ferrous iron chelating activity and DPPH. radical scavenging activity.
Synthesis of 1-(3-arylimino-4-aryl-5-imino-1,2,4-thiadiazolidine)-3-tetra-O-benzoyl-β-D-glucosyl carbamides were realized by successful oxidation of aryl thiocarbamides into 3-arylimino-4-aryl-5-imino-1,2,4-thiadiazolidines (IIac), (so called Hector's base) by using hydrogen peroxide in ethanolic medium, which on reacting with tetra-Obenzoyl- β-D-glucosyl isocyanate (I) produces a new series of 1-(3-arylimino-4-aryl-5-imino-1,2,4-thiadiazolidine)- 3-tetra-O-benzoyl-β-D-glucosyl carbamides (IIIa-c). The newly synthesized compounds have been characterized by usual chemical transformations and IR spectral analysis.The polarimetric study of the compounds has been carries out.
Several 3-hepta-O-acetyl-β-D-maltosylimino-5-arylimino-1,2,4-dithiazolidine hydrobromides (IV a-g) have been synthezed by debenzylation and cyclization of 1-aryl-5-hepta-O-acetyl-β-D-maltosyl-2-S-benzyl-2,4-isodithiobiurets with bromine in chloroform. The identities of these newly synthesized compounds were established on the basis of elemental analysis an IR, 1HNMR and Mass spectral analysis.
To discover new 1,3,4-thiadiazoles derivatives which may possess significant biological activities, we synthesized a series of novel 3-Substituted-6-aryl-1,2,4-triazolo [3,4-b][1,3,4] thiadiazoles. All the synthesized title compounds were characterized by elemental analysis, IR, 1H-NMR. Crop protective activity tests showed that these compounds have remarkable effects on the growth of crop.
A series of 2,4-disubstituted thiazole derivatives (6a-k) were synthesized by a condensation reaction between 2-amino, 4-substituted phenyl thiazole and 2-(2,3-dimethylanilino)benzoic acid. The structure of synthesized thiazole derivatives 6(a-k) were characterized by using IR, NMR, Mass Spectroscopy and evaluated for their in vitro anti-inflammatory activity using albumin denaturation method and compared with standard drug diclofenac sodium. The compounds 2-(2,3-dimethyl phenylamino)-N-(4-(4-methyl phenyl) thiazol-2-yl)benzamide (6a) and 2-(2,3-dimethyl phenylamino)-N-(4-(4-nitrophenyl) thiazol-2-yl)benzamide (6c) showed better anti-inflammatory activity when compared with a standard drug.
Viscosity measurement of 1,3-diaryl carbamides was carried out in different binary solvent mixtures. The study was implemented for several variations in percentage of binary solvents, variation in concentration of solute in binary solvents as well as variation in temperatures. Using above data relative viscosity, excess viscosity and thermodynamic parameters i.e. enthalpy, entropy and gibbs free energy have been computed. Thermodynamic parameters and viscosity have been calculated to interpret molecular interaction.
1, 3-thiazines are prepared by refluxing the mixture of 2-Hydroxy-3-bromo/nitro -5-chlorochalcone and phenylthiourea in alcohol and aq.KOH medium. The newly synthesized 1,3-thiazenes were characterized on the basis of elemental analysis and spectroscopic data of IR,NMR. The melting points were taken in an open capillary tube. All compounds have been evaluated for their in vitro growth of inhibitory activity againstEscherichia coli, Staphylococcus aureaus, Bacillus subtilis and Phaseolusargenosa.
Refractive indices of binary liquid mixtures and 1, 3 diaryl carbamides in different percentage of binary liquid mixture such as acetone-water, dioxane-water & DMSO-water at 27± 0.1°C were measured by Abbes' refractrometer. The data obtained was utilized to calculate molar refraction & polanzability constant which explain solute-solvent, solvent-solvent interactions.
Thiadiazole is a heterocyclic molecule made up of one sulphur atom, two nitrogen atoms, and two double-bonded 5- membered ring systems. Heterocyclic compounds having biological activity serve a significant role in medicinal chemistry. More than one or two heteroatoms are also included in the five-membered ring, including thiadiazole, oxazole, thiazole, azole, pyrrole, triazine, and others. Thiadiazole has been shown to have anticancer, antiinflammatory, anti-diabetic, antimicrobial, antifungal, antibacterial, antiviral, anti-tuberculosis, anticonvulsant, antidepressant, antileishmanial, and other biological effects.
1,4-dihydropyridine (DHPs) is a class of compounds that are significantly present in a variety of natural products
and commercial medicines such as felodipine. This study aims to modify cinnamaldehyde to become derivatives of
1,4-dihydropyridine using NiFe2O4 MNPs as the catalyst. NiFe2O4 MNPs were synthesized by the co-precipitation
method using a 2:1 molar ratio between ferrite nitrate and nickel nitrate and analyzed by XRD and SEM-EDX. The
results of the characterization support that NiFe2O4 MNPs were successfully synthesized. After that, NiFe2O4 was
tested for its ability as a catalyst in the synthesis of 1,4 dihydropyridine. The synthesis results are confirmed with
MP apparatus, UV/Vis Spectrophotometry, FT-IR and GC-MS, and obtained three 1,4-dihydropyridine compounds,
namely 2,6-dimethyl-4-phenyl-1,4-dihydropyridine-3,5-dicarboxylic acid diethyl ester (compound 1), 2,6-dimethyl4-styryl-1,4-dihydropyridine-3,5-dicarboxylic acid diethyl ester (compound 2), and 4-(4-Hydroxy-phenyl)-2,6-
dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid diethyl ester (compound 3). The ability NiFe2O4 as catalyst
gives a significant difference yield between the reaction with and without the catalyst.
Thioamido, quinilineo, benzamido and benzoido group containing heterocycles created their own identity and importance in pharmaceutical, medicinal, agricultural and drug sciences. Thioamido and benzamido heterocyclic compounds showed noticeable and remarkable applications in industrial, pharmaceutical, medicinal and drug chemistry. Hence taking all these facts into consideration it was thought interesting to synthesize N-(7- substitutedthiocarbamidoquinoline-4-yl)-N,N-diethyl-pentane-1,4-diamines by interacting N-(7-chloroquinoline-4- yl)-N,N-diethyl-pentane-1,4-diamine with various thiourea in isopropanol medium. The justification and identification of the structure of these newly synthesized compounds had been established on the basis of chemical characterization, elemental analysis and through spectral data The antimicrobial activities of this compounds were screened against E. coli, S. typhi, S. abony, P. aeruginosa, B. subtilis, A. niger, and C. albicons pathogens which are hither to unknown.
The work reports derivatives of 2-amino-4-(2-chloro-5-(4-substituted phenyl) pyridine-3-yl)-1-(4- substitutedphenyl)-7,7-disubstituted-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carbonitrile Q(1-14) have been synthesized by the reaction of 5,5-disubstituted-1, 3-cyclohexanedione and 4- substituted aniline in the presence of ethanol and piperidine. The structure of synthesized compounds is characterized by spectroscopic methods suchas IR, 1H NMR, Mass Spectroscopy, and elemental analysis. The efficient novel derivativesQ(1-14) with different effective substituent (-CH3, -NO2, -OCH3 , -Br) was screened against antibacterial and antifungal effectively and showednotable action against tested microbes.
A series of novel methylene-bis-8-substituted [1,5]-benzothiazepines 4 was prepared by the reaction of methylene-bis-chalcones-3 with 2-amino-5-methyl-thiophenol.The structures of the synthesized compounds were confirmed by their IR, 1H, 13C NMR and Mass spectral analyses. All the synthesized compounds were tested for their antimicrobial activity against Gram-positive, Gram-negative bacteria and fungi. Among the synthesized compounds, the compounds 4f, and 4g, were found to be the most active against Bacillus subtilis, Bacillussphaericus, Staphylococcus aureus, Klebsiella aerogenes and Chromobacterium violaceum. Similarly thesecompounds showed potent antifungal effect against Candida albicans, Aspergillus fumigatus, Trichophytonrubrum, and Trichophyton mentagrophytes. It is interesting to note that the compounds with heterocyclic ring substituents at the 4th position of benzothiazepine system displayed notable antibacterial activity, almost equal to that of streptomycin and penicillin.
The (E)-1,5-diphenylcarbazone cobalt(II) [CoIIArNNCONNAr] was synthesized by addition of (E)-1,5-diphenylcarbazone 2[ArNHNHCO=NAr] to cobalt diacetate with reflex to 24 hrs. The kinetics of oxidation of Cobalt(II) of [CoIIArNNCONNAr] by N-chloro-p-toluenesulphonamide Chloramine-T to Cobalt(III) have been investigated at 25°C. The reaction is consecutive first order with respect to both [Cobalt(II)Complex] and Chloramine-T. The order of the reaction in [H+] was fractional and the rate constant was unaffected by the ionic strength. Rate law of the suggested mechanism including all factors affecting the rate of reaction was derived.