Thieno[2,3-b]pyridine derivatives are potent anti-platelet drugs, inhibiting platelet activation, aggregation and showing synergy with aspirin

Eur J Med Chem. 2018 Jan 1:143:1997-2004. doi: 10.1016/j.ejmech.2017.11.014. Epub 2017 Nov 7.

Abstract

Drugs which inhibit platelet function are commonly used to prevent blood clot formation in patients with Acute Coronary Syndromes (ACS) or those at risk of stroke. The thieno[3,2-c]pyridine class of therapeutic agents, of which clopidogrel is the most commonly used, target the P2Y12 receptor, and are often used in combination with acetylsalicylic acid (ASA). Six thieno[2,3-b]pyridine were assessed for in vitro anti-platelet activity; all derivatives showed effects on both platelet activation and aggregation, and showed synergy with ASA. Some compounds demonstrated greater activity when compared to clopidogrel. These compounds, therefore, represent potential novel P2Y12 inhibitors for improved treatment for patients.

Keywords: Aspirin; Clopidogrel; Platelets; Thienopyridine; Thrombosis.

MeSH terms

  • Adult
  • Aspirin / chemistry
  • Aspirin / pharmacology*
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • Male
  • Molecular Structure
  • Platelet Activation / drug effects
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / chemical synthesis
  • Platelet Aggregation Inhibitors / chemistry
  • Platelet Aggregation Inhibitors / pharmacology*
  • Pyridines / chemical synthesis
  • Pyridines / chemistry
  • Pyridines / pharmacology*
  • Structure-Activity Relationship
  • Young Adult

Substances

  • Platelet Aggregation Inhibitors
  • Pyridines
  • thieno(2,3-b)pyridine
  • Aspirin