Synthesis and structure-activity relationship of potent bicyclic lactam thrombin inhibitors

Bioorg Med Chem Lett. 1999 Apr 5;9(7):913-8. doi: 10.1016/s0960-894x(99)00130-4.

Abstract

A simple and versatile method for preparation of (D)-Phe-Pro peptidomimetic bicyclic thiazolidine lactams is presented. These bicyclic lactams have chemical diversity alpha to the lactam carbonyl and, when linked to electrophilic arginines, provide potent thrombin inhibitors.

MeSH terms

  • Antithrombins / chemical synthesis*
  • Antithrombins / chemistry
  • Antithrombins / pharmacology
  • Bridged Bicyclo Compounds / chemical synthesis
  • Bridged Bicyclo Compounds / chemistry
  • Bridged Bicyclo Compounds / pharmacology
  • Lactams / chemical synthesis
  • Lactams / chemistry
  • Lactams / pharmacology
  • Structure-Activity Relationship

Substances

  • Antithrombins
  • Bridged Bicyclo Compounds
  • Lactams