SUBSTITUTED CARBOXAMIDE ANALOGUES AS A NEW CLASS OF LOCAL ANESTHETIC AGENTS: SYNTHESIS AND BIO-EVALUATION

Abstract: A series of N-(2-oxo-2-(phenylamino) ethyl) substituted-4-carboxamide derivatives were synthesized as local anesthetic agents. The structures of carboxamide derivatives were established on the basis of IR, and 1H spectral data. All the compounds were subjected to surface local anesthetic activity assay and infiltration local anesthetic activity assay. Among the tested compounds, N-(2-oxo-2-(p-tolylamino) ethyl) piperidine-1-carboxamide (4h) and N-(2-((4-methoxyphenyl) amino)-2-oxoethyl) piperidine-1-carboxamide (4m) were most promising compounds in terms of surface local anaesthetic and infiltration local anaesthetic activity on rats having considerably lower liver toxicity. Keywords: Carboxamide, surface local anesthetic activity, infiltration local anesthetic activity, hepatotoxicity.