Synthesis and anti-platelet evaluation of 2-benzoylaminobenzoate analogs

Bioorg Med Chem. 2008 May 15;16(10):5803-14. doi: 10.1016/j.bmc.2008.03.071. Epub 2008 Mar 31.

Abstract

Fifty-two 2-benzoylaminobenzoate analogs were synthesized and subjected to anti-platelet aggregation assay using arachidonic acid (AA), collagen (Col), thrombin (Thr), and U46619 as inducers. The results revealed that most of 2-benzoylaminobenzoic acid derivatives showed a selectively inhibitory effect on AA-induced platelet aggregation. As a result of the 2-benzoylaminobenzoic acid derivatives (18, 44, and 46), there were no inhibitory effects on platelet aggregation induced by U46619, but these elicited an inhibitory effect on thromboxane B(2) formation at 1.0microM. These 2-benzoylaminobenzoate analogs were therefore proposed as cyclooxygenase inhibitors.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminobenzoates / chemical synthesis*
  • Aminobenzoates / chemistry
  • Aminobenzoates / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Evaluation, Preclinical
  • Humans
  • Inhibitory Concentration 50
  • Molecular Structure
  • Platelet Aggregation / drug effects*
  • Platelet Aggregation Inhibitors / chemical synthesis*
  • Platelet Aggregation Inhibitors / chemistry
  • Platelet Aggregation Inhibitors / pharmacology*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Aminobenzoates
  • Platelet Aggregation Inhibitors