SYNTHESIS AND BIOLOGICAL-ACTIVITY OF P-2-P-4 AZAPEPTIDOMIMETIC P-1-ARGININAL AND P-1-KETOARGININAMIDE DERIVATIVES - A NOVEL CLASS OF SERINE-PROTEASE INHIBITORS

Authors
SEMPLE JE ROWLEY DC BRUNCK TK RIPKA WC
Citation
Je. Semple et al., SYNTHESIS AND BIOLOGICAL-ACTIVITY OF P-2-P-4 AZAPEPTIDOMIMETIC P-1-ARGININAL AND P-1-KETOARGININAMIDE DERIVATIVES - A NOVEL CLASS OF SERINE-PROTEASE INHIBITORS, Bioorganic & medicinal chemistry letters, 7(3), 1997, pp. 315-320
Citations number
35
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
3
Year of publication
1997
Pages
315 - 320
Database
ISI
SICI code
0960-894X(1997)7:3<315:SABOPA>2.0.ZU;2-9
Abstract
Molecular modeling and topographic considerations of the thrombin-spec ific sequences Boc-Asp-Pro-Arg-TS or Ac-d-Phe-Pro-Arg-TS (TS = transit ion state analog electrophilic center) and related scaffolds led to th e design of novel P-2-P-4-azapeptidomimetic P-1-argininal and P-1-keto argininamide derivatives (3a-j). The synthesis and biological activity of these potential serine protease inhibitors are presented. (C) 1997 , Elsevier Science Ltd.