Synthesis of Some Azoles Incorporating a Sulfonamide Moiety as Anticonvulsant Agents

Abstract

Many derivatives of heterocyclic compounds containing a sulfonamide thiazole moiety were synthesized through the reaction of 2-(cyano or chloro)-N-(4-(N-thiazol-2-ylsulfamoyl)phenyl)acetamide with isocyanate followed by halogenated compounds, arylidene, 2-hydroxy benzaldehydes, active methylene compounds, and heterocyclic amines. The anticonvulsant activity for 15 of the synthesized compounds was evaluated and 6 compounds showed protection against picrotoxin-induced convulsion. 4-(6-Amino-3,5-dicyano-4-(4-methoxyphenyl)-2-oxopyridin-1(2H)-yl)-N-(thiazol-2-yl)benzenesulfonamide (11b) exhibited significant anticonvulsive effects, abolished the tonic extensor phase and offered 100% protection.