SYNTHESIS AND BIOLOGICAL EVALUATION OF BENZOTHIAZOLE DERIVATIVES OF PYRIMIDINES,ACRYLONITRILES,AND COUMARINS

摘要

A number of benzothiazole derivatives of 2-aminopyrimidines (3a-b,5,6a-b,and 7),benzothiazole-3-arylacrylonitriles (10 a-c),and benzothiazol-2-yl-coumarins (18a c,and 20) were synthesized by reacting benzothiazole derivatives with dicarbonyl compounds,and aromatic aldehydes.The unexpected 2-(4-methoxyphenyl)benzo[d]thiazole (14) was obtained as a unique product via the reaction of 2-aminothiophenol with ethyl 3-(4-methoxyphenyl)-2-scyanoacrylate.2-(Benzo[d]thiazol-2-yl)-3-(4-hydroxyphenyl)acrylonitrile (10a) exhibited activity against Staphylococcus aureus.2-(Benzo[d]thiazol-2-ylamino)pyrimidine-4,6-(1H,5H)-dione (3b) showed antibacterial activity selectivity against Corynebacterium xerosis.2-(Benzo[d]thiazol-2-ylamino)-6-methylpyrimidin-4(3H)-one (5) showed weak anti-fungal activity against Candida albicans.