Prostaglandin Synthetase Inhibitors

  • T. Y. Shen
Part of the NATO Advanced Study Institutes Series book series (NSSA, volume 13)


Since the discovery of aspirin and indomethacin as prostaglandin synthesis inhibitors in 1971 (1), within a short span of five years, literally hundreds of chemical structures have been reported as inhibitors of the prostaglandin synthetase system. These compounds, either as therapeutic agents or as research tools, have become a new class of pharmacological agents. Standard drugs such as indomethacin and aspirin, have been used widely and effectively in delineating the involvement of prostaglandins in various biological phenomena. The general correlation of PG synthetase inhibitory activity and antiinflammatory property in many cases has stimulated an active search for new synthetase inhibitors as potential antiarthritic agents. Recently, notable advances were made in several aspects, which not only facilitated the search for new inhibitors, but also suggested possible directions for further improvements. In this communication some notable chemical features of PG synthetase inhibitors will be reviewed briefly. Some of our findings with two new antiarthritic drugs, sulindac and diflunisal, will be highlighted to illustrate the influence of chemical and pharmacokinetic properties on the safety and selectivity of PG synthetase inhibitors.


Synthetase Inhibitor Prostaglandin Biosynthesis Prostaglandin Synthetase Prostaglandin Synthetase Inhibitor Sulindac Sulfide 
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Copyright information

© Plenum Press, New York 1977

Authors and Affiliations

  • T. Y. Shen
    • 1
  1. 1.Merck Sharp & Dohme Research LaboratoriesRahwayUSA

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