SYNTHESIS OF SOME N-ARYLAZOLE ACETAMIDE DERIVATIVES AND THEIR ANTICONVULSANT AND ANTIMICROBIAL ACTIVITIES

Some new N-arylazole acetamide derivatives have been prepared by the r eaction of alpha-bromo-N-arylacetamide with imidazole, pyrazole and 1, 2,4-triazole. The structures of these compounds have been confirmed by UV,IR, H-1-NMR and elementary analysis. Their anticonvulsant activiti es were determined by maximal electroshock (MES) and subcutaneous metr azol (Scmet) tests. Most of the compounds showed anticonvulsant activi ty with significantly low neurotoxicity according to Phase I tests. Co mpound 6 carrying alpha-naphthyl and 1,2,4-triazole was found active i n the MES test with ED(50) = 64.9 mg/kg and TD (50)= 221.0 mg/kg but i t was not active in corneally stimulated rats. Antibacterial and antif ungal activities of the compounds were detemined against S. aureus, E. coli, P. aeruginosa, C. albicans, C. parapsilosis, C. pseudotropicali s and C. stellatoidea by using the microdilution broth method. Compoun ds 8 and 10 showed significant activity (MIC < 32 mu g/ml) against var ious Candida species.