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Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors

✍ Scribed by J.Edward Semple; David C. Rowley; Terence K. Brunck; William C. Ripka

Publisher
Elsevier Science
Year
1997
Tongue
English
Weight
388 KB
Volume
7
Category
Article
ISSN
0960-894X

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✦ Synopsis

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 P2-P4-azapeptidomimetic Pl-argininal and Pl-ketoargininamide derivatives (3a-j). The synthesis and biological activity of these potential serine protease inhibitors are presented.

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