[Synthesis and antiplatelet activity of 2-amino-4,5-diphenylthiazole derivatives].
A series of 4,5-diphenylthiazoles containing morpholinoalkyl amino groups at the 2 position was synthesized and their anti-platelet activities were evaluated. The inhibitory effects of the compounds in which phenyl groups at the 4 position were substituted by methoxy groups were more potent than those of aspirin and ibuprofen on the collagen-induced rabbit platelet aggregation. These compounds were also shown to have potent efficacies on the arachidonic acid-induced platelet aggregation. On the other hand, these compounds did not affect the ADP-induced platelet aggregation similarly to non-steroidal anti-inflammatory agents. Moreover, their efficacies on the inhibition of prostaglandin synthesis were more potent than that of ibuprofen. Therefore, we thought that 2-(morpholinoalkyl)amino-4,5-diphenylthiazoles, in spite of their basic properties, inhibited the platelet aggregation based on cyclooxygenase.
D000244:Adenosine Diphosphate / Q000037:antagonists & inhibitors; D000818:Animals; D016718:Arachidonic Acid / Q000037:antagonists & inhibitors; D002478:Cells, Cultured; D003094:Collagen / Q000037:antagonists & inhibitors; D016861:Cyclooxygenase Inhibitors; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D011817:Rabbits; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D016861:Cyclooxygenase Inhibitors; D010975:Platelet Aggregation Inhibitors; D013844:Thiazoles; D016718:Arachidonic Acid; D000244:Adenosine Diphosphate; C002886:Bax 439; D003094:Collagen