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Synthesis and biological activity of P2–P4azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
7
Issue
3
Identifiers
DOI: 10.1016/s0960-894x(97)00005-x
Disciplines
  • Biology
  • Design

Abstract

Abstract Molecular modeling and topographic considerations of the thrombin-specific sequences Boc-Asp-Pro-Arg-TS or Ac-d-Phe-Pro-Arg-TS (TS = transition state analog electrophilic center) and related scaffolds led to the design of novel P 2–P 4-azapeptidomimetic P 1-argininal and P 1-ketoargininamide derivatives ( 3a-j). The synthesis and biological activity of these potential serine protease inhibitors are presented.

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