A series of new benzothiazole derivatives were synthesized and evaluated for anti-inflammatory and anti-diabetic activity. The structures of the compounds were confirmed by 1H-NMR,13C-NMR, FT-IR, and LC-MS. Among the all synthesized compounds, 4a showed very good anti-inflammatory activity. The compounds 3a, 3c, 3d, 5b also showed good anti-inflammatory activity. In anti-diabetic studies, the compounds 5a, 5b, and 3d showed moderate alphaamylase inhibition activity.