Inhibition of platelet aggregation by novel triphenylethylene analogs.
The present study has evaluated the effect of some newly synthesized triphenylethylene (TPE) analogs on platelet arachidonic acid metabolism and function. All compounds tested inhibited arachidonic acid induced platelet aggregation and several were superior to aspirin in their relative potency. Introduction of a carboxyl function into the alpha-ring, which should enhance binding according to proposed structural models for cyclooxygenase inhibitors, was not found to be beneficial. Increased structural rigidity, which resulted from covalent linkage of two aromatic rings in this series, did not eliminate anti-aggregatory properties.
D000328:Adult; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000097:blood; D001792:Blood Platelets / Q000378:metabolism; D002227:Carbazoles / Q000138:chemical synthesis / Q000494:pharmacology; D005260:Female; D006801:Humans; D007700:Kinetics; D008297:Male; D008861:Microsomes / Q000187:drug effects / Q000378:metabolism; D009570:Nitriles / Q000138:chemical synthesis / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects*; D013267:Stilbenes / Q000138:chemical synthesis / Q000494:pharmacology*
D001095:Arachidonic Acids; D002227:Carbazoles; D009570:Nitriles; D013267:Stilbenes; D016718:Arachidonic Acid