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Highly selective tripeptide thrombin inhibitors

R T Shuman1, R B Rothenberger, C S Campbell

  • 1Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285.

Journal of Medicinal Chemistry
|February 5, 1993
PubMed
Summary
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Researchers designed novel tripeptide aldehydes that potently inhibit thrombin, a key enzyme in blood clotting. These selective thrombin inhibitors show promise as pharmacological tools and potential therapeutic agents for antithrombotic applications.

Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Tripeptide aldehydes, exemplified by Boc-D-Phe-Pro-Arg-H (51), are direct inhibitors of thrombin.
  • Serine protease inhibitors are valuable pharmacological tools and potential therapeutic agents.

Purpose of the Study:

  • To discuss structure-activity relationships (SAR) of anticoagulant peptides with high selectivity for thrombin.
  • To investigate the role of the amino acid residue in position 1 of tripeptide aldehydes.
  • To develop potent and selective serine protease inhibitors.

Main Methods:

  • Synthesized and evaluated a series of di- and tripeptide arginine aldehydes.
  • Investigated structural and conformational roles via amino acid substitutions.
  • Assessed in vitro inhibitory effects against thrombin, trypsin, plasmin, factor Xa, and tissue plasminogen activator.

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Main Results:

  • Many synthesized peptides demonstrated potent antithrombotic activity.
  • High selectivity toward thrombin was observed for several compounds.
  • Compound 5f (D-1-Tiq-Pro-Arg-H.sulfate) emerged as a highly active and selective tripeptide aldehyde inhibitor of thrombin.

Conclusions:

  • The study provides insights into designing potent and selective serine protease inhibitors.
  • Novel tripeptide aldehydes exhibit significant antithrombotic potential.
  • Compound 5f represents a promising lead for further development of clinically useful antithrombotic agents.