Relationship between structure and activity of aspirin-related compounds on the inhibition of in vitro platelet aggregation

Farmaco Sci. 1986 Mar;41(3):205-14.

Abstract

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.

MeSH terms

  • Adenosine Diphosphate / pharmacology
  • Arachidonic Acid
  • Arachidonic Acids / pharmacology
  • Aspirin / pharmacology*
  • Collagen / pharmacology
  • Drug Interactions
  • Humans
  • In Vitro Techniques
  • Platelet Aggregation / drug effects*
  • Salicylates / pharmacology
  • Structure-Activity Relationship

Substances

  • Arachidonic Acids
  • Salicylates
  • Arachidonic Acid
  • Adenosine Diphosphate
  • Collagen
  • Aspirin