RATIONAL DESIGN AND SYNTHESIS OF A NOVEL, SELECTIVE CLASS OF THROMBININHIBITORS - P-1-ARGININAL DERIVATIVES INCORPORATING P-3-P-4 QUATERNARY LACTAM DIPEPTIDE SURROGATES

Authors
SEMPLE JE MINAMI NK TAMURA SY BRUNCK TK NUTT RF RIPKA WC
Citation
Je. Semple et al., RATIONAL DESIGN AND SYNTHESIS OF A NOVEL, SELECTIVE CLASS OF THROMBININHIBITORS - P-1-ARGININAL DERIVATIVES INCORPORATING P-3-P-4 QUATERNARY LACTAM DIPEPTIDE SURROGATES, Bioorganic & medicinal chemistry letters, 7(18), 1997, pp. 2421-2426
Citations number
31
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
18
Year of publication
1997
Pages
2421 - 2426
Database
ISI
SICI code
0960-894X(1997)7:18<2421:RDASOA>2.0.ZU;2-Z
Abstract
SAR and molecular modeling investigations on the potent and selective thrombin inhibitor 1b (CVS 1578) and related serine protease inhibitor s led to the design of series 2a-g, featuring quaternary alpha-amino-a lpha-benzyl-lactam scaffolds that serve as novel P-3-P-4 dipeptide mim ics. The design, synthesis, and biological activity of these targets a re presented. (C) 1997 Elsevier Science Ltd.