Studies on the synthesis and COX-2 inhibitory activities of some 6-(Thiazole-4-yl) 2-Oxo-3H-Benzothiazole derivatives

In this study, we aimed to synthesize bearing 2,4-diarylthiazole position 6 of 2-oxo-3H-benzothiazole derivatives which have decreased unexpected effects and have equal or more antiinflamatory activity compared with NSAIDs. In this study, 6-(substitue phenyl-1,3- thiazol-4-yl)-2-oxo-3H-benzothiazoles (compounds 1-6), ethyl [6- (substituephenyl)-1,3-thiazol-4-yl)-2-oxo-3H-benzothiazol-3-yl]acetates (compounds 7-12) and [6-(substituephenyl)-1,3-thiazol-4-yl)-2-oxo-3Hbenzothiazol- 3-yl] acetic acids (compounds 13-18) structured compounds, which might have selective COX-2 inhibitory and TxA2 synthase inhibitory activities, are synthesized. The COX-1 and COX-2 inhibitory activity of the synthesized compounds were investigated by using one of in vitro test system, the ELISA method. We used SC-560 as a reference for COX-1 inhibitory activity and DuP-697 for COX-2 inhibition activity. We observed that the compounds carrying acetic acid or ester moiety at position 3 in the 2-oxo-3H-benzothiazole ring system had higher COX-1 inhibitory activity. Besides, COX-2 inhibition activity was observed in 4-flourophenyl substituted compounds. Key Words: Thiazole, 2-oxo-3H-benzothiazole, selective COX-2 inhibitors, microwaves irradiation in organic synthesis