Journal of Chemical and Pharmaceutical Research

ABSTRACT 3,5-bistrifluor omethylphenyl-1,3,4-oxadiazolethiol was obtained from the reaction of hydrazide derivative with carbondisulphide in basic media, which was alkylated in to nitrile derivative. Nitrile compound 3 undergoes pinner reaction using dry methanolic HCl to abtained imidoether hydrochloride salt 4. Which was further react with 2-aminoethanol, cysteamine, ethylenediamine, semicarbazide, thiosemicarbazide, 2-aminophenol, 2-aminothiphenol, orthophenylenediamine, to give substituted oxazoline, thiazoline, imidazoline, triazolone, triazolethiol, benzoxazoles, benzothiazoles and benzimidazoles derivative respectively. Conversion of sulphide to sulphoxide was achieved by oxidation with m-CPBA (Compounds 8a-8l). All newly synthesized compounds screened for their antimicrobial activity. The antibacterial activity revealed that all compounds screened to showed good or moderate activity.

Abstract  Quantitative activity relationship (QSAR) has been carried out in a series of 1,5-di(4-amidino phenoxy) pentane & its analogues against Topoisomerase II inhibitory activities. The 2D QSAR studies activity is negatively influenced by the presence of linker (O or N), contribution of hydrophobicity and substitution on para position contributed in molar refractivity. The best QSAR model with good correlation coefficient (r 2 =0.712), of high statistical significance (> 99.9%) well explained the variance in activity.

Abstract   A series of substituted 1, 4-Dihydropyridine derivatives were synthesized and the structures of these compounds were established on the basis of spectral and elemental analysis. All the compounds were evaluated for anti convulsant activity by Maximal Electroshock Induced convulsions in Rats, PTZ induced convulsions in Rats, and Strychnine induced Convulsions in Rats methods. Compounds A 1 ,A 2 ,A 3 ,A 4 ,B 1 ,B 2 ,B 3 ,B 4 have been found to exhibit anti convulsant activity For more info: http://www.jocpr.com/articles/synthesis-and-evaluation-of-some-new-substituted-14dihydro-pyridine-derivatives-and-their-anticonvulsant-activity.pdf