Design, synthesis and in vivo anticonvulsant screening in mice of Novel phenylacetamides

A set of seven novel N-substituted 2-anilinophenylacetamides were designed by pharmacophore generation and using flexible alignment module of MOE software. The novel molecules were synthesized and screened for anticonvulsant activity in Swiss albino mice by MES and ScPTZ induced seizure tests. Test compounds were found to be potent in MES test. Compounds 12 and 14 were found to be more potent with ED50 values 24.0 and 8.0 mg kg–1, respectively, and their activity was comparable to standard drugs (Phenytoin, Carbamazepine). Test compounds did not show significant activity in ScPTZ test. Compounds 12 and 14 also exhibited higher protective indices (20.3 and 87.5, respectively) when assessed for neurotoxicity by rotarod test as compared to the standards.

Seven novel 2-anilinophenylacetamides designed by pharmacophore generation and flexible alignment were synthesized. Compounds 12 and 14 displayed potent anticonvulsant activity (ED50 values of 24.0 and 8.0 mg kg–1, respectively) in MES test and also exhibited higher protective indices compared to standard drugs.Figure optionsDownload as PowerPoint slide