Abstract
Keeping in view the successive attributes of benzodiazepines on the central nervous system, we have synthesized a novel series of benzodiazepine derivatives as antioxidant and anxiolytic agents. All the compounds were obtained in good yield by facile synthesis. To check their antioxidant potential, DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging assay was performed. Among all the synthetics seven derivatives (SD-3, SD-5, SD-7, SD-14, SD-18, SD-19, and SD-20) exhibited IC50 values ranging from 76 to 489 nM. These seven compounds were further evaluated to check their binding abilities towards the benzodiazepine binding site on GABAA receptors. Three best-fit ligands (SD-3, SD-14 and SD-20) were further evaluated for their anxiolytic effect by using three in vivo mice models i.e. Elevated Plus Maze, Light & Dark box, and Mirror Chamber model. The study revealed that compounds SD-3 and SD-20 showed the best anxiolytic effect as compared to standard drug diazepam even at an oral dose of 1.0 mg/kg.
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