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.