Relationship between structure and activity of aspirin-related compounds on the inhibition of in vitro platelet aggregation.
Thirteen aspirin-related compounds were tested for inhibitory activity on platelet aggregation in human platelet rich plasma (PRP) induced with ADP, collagen and arachidonic acid. The following structure-activity relationships were found: none of the functional groups used to replace the acetyl group retained the significant antiaggregant activity of aspirin; anti-aggregant activity was enhanced when the carboxylic group was replaced with a hydroxyl or an acetylated hydroxyl group. The activity of these mono and diacetylated pyrocatechol derivatives was unaffected by incubation of PRP with sodium salicylate.
D000244:Adenosine Diphosphate / Q000494:pharmacology; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000494:pharmacology; D001241:Aspirin / Q000494:pharmacology*; D003094:Collagen / Q000494:pharmacology; D004347:Drug Interactions; D006801:Humans; D066298:In Vitro Techniques; D010974:Platelet Aggregation / Q000187:drug effects*; D012459:Salicylates / Q000494:pharmacology; D013329:Structure-Activity Relationship
D001095:Arachidonic Acids; D012459:Salicylates; D016718:Arachidonic Acid; D000244:Adenosine Diphosphate; D003094:Collagen; D001241:Aspirin