SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF FEW 2-(SUBSTITUTED ARYL)-4-(HETEROARYL)-2,3-DIHYDRO-1H-1,5-BENZODIAZEPINE DERIVATIVES
Abstract
Benzodiazepines represent a class of privilege scaffold in the modern era of medicinal chemistry as central nervous system active agents. The present work reported synthesis of a series of 2-(substituted aryl)-4-(heteroaryl)-2,3-dihydro-1H-1,5-benzodiazepines. Structural characterization of title compounds was done by using analytical techniques such as IR and 1H-NMR. An acute toxicity study was done to determine the LD50 of the compounds. The compounds were subjected to pharmacological studies to evaluate anticonvulsant potential in mice by strychnine-induced convulsions method. The pharmacological evaluation of the compounds showed an increase in latency (onset time) to induce convulsions and a decrease in convulsions compared to control. The compounds B3, B6 and B8 showed the highest percentage protection as 80% with latency to induce convulsions as 6.46, 6.35 and 6.12 minutes, respectively compared to control at 3 mg/kg. The structural features analysis revealed that the phenyl ring’s second position substituted with halogen, hydroxy group of 2-(substituted phenyl)-4-(furan-2-yl/thiophene-2-yl)-2,3-dihydro-1H-1,5-benzodiazepine enhanced the anticonvulsant potential of the compounds.
Keywords:
Anticonvulsant, 1,5-benzodiazepine, chalcone, strychnine induced convulsions, o-phynelene diamine, 2-acetylfuran, 2-acetylthiopheneDOI
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