Thromboxane A2 synthetase inhibitors. I. Syntheses and activities of various N-heteroaromatic derivatives.

Basic N-heteroaromatic derivatives (1, 2, 4-triazole, thiazole and pyrimidine derivatives) having a 2-[4-(carboxy)phenoxy]ethyl moiety or a 4-[2-(carboxy)vinyl]benzyl moiety were prepared, and evaluated for ability to inhibit thromboxane A2 (TXA2) synthesis. Among the compounds prepared in this study, the 5-substituted thiazole derivatives 14d, 27 and 28 were more potent inhibitors of TXA2 production than the corresponding imidazole derivatives, and the 1-substituted 1H-1, 2, 4-triazole derivatives 14a and 15a were almost as potent as the corresponding imidazole derivatives.