Progress in 5H[1]benzopyrano[4,3-d]pyrimidin-5-amine series: 2-methoxy derivatives effective as antiplatelet agents with analgesic activity

Farmaco. 2002 Sep;57(9):753-8. doi: 10.1016/s0014-827x(02)01269-7.

Abstract

A series of 2-methoxy-5H[1]benzopyrano[4,3-d]pyrimidin-5-amines were prepared and screened for their in vitro antiplatelet activity inducing the aggregation by ADP, arachidonic acid (AA) and collagen. In vivo experiments were performed in order to evaluate their antiphlogistic, analgesic and antipyretic activities. Title compounds showed antiplatelet activity in aggregation AA or collagen-induced, and a good analgesic activity without any gastric toxicity. Comparison with a number of analogue benzopyrano[4,3-d]pyrimidine derivatives and some SAR consideration were reported.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Diphosphate
  • Analgesics, Non-Narcotic / chemical synthesis*
  • Analgesics, Non-Narcotic / pharmacology
  • Analgesics, Non-Narcotic / toxicity
  • Animals
  • Arachidonic Acid
  • Collagen
  • Gastric Mucosa / drug effects
  • Guinea Pigs
  • Mice
  • Pain Measurement
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / chemical synthesis*
  • Platelet Aggregation Inhibitors / pharmacology
  • Platelet Aggregation Inhibitors / toxicity
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology
  • Pyrimidines / toxicity
  • Rats
  • Structure-Activity Relationship

Substances

  • Analgesics, Non-Narcotic
  • Platelet Aggregation Inhibitors
  • Pyrimidines
  • Arachidonic Acid
  • Adenosine Diphosphate
  • Collagen