DESIGN AND SYNTHESIS OF CONFORMATIONALLY CONSTRAINED ARGINAL THROMBININHIBITORS

Authors
SALIMBENI A PALEARI F CANEVOTTI R CRISCUOLI M LIPPI A ANGIOLINI M BELVISI L SCOLASTICO C COLOMBO L
Citation
A. Salimbeni et al., DESIGN AND SYNTHESIS OF CONFORMATIONALLY CONSTRAINED ARGINAL THROMBININHIBITORS, Bioorganic & medicinal chemistry letters, 7(17), 1997, pp. 2205-2210
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
17
Year of publication
1997
Pages
2205 - 2210
Database
ISI
SICI code
0960-894X(1997)7:17<2205:DASOCC>2.0.ZU;2-S
Abstract
A series of conformationally constrained arginal thrombin inhibitors w as prepared starting from 5,6 or 5,7 bicyclic lactamic structures, tha t an indirect approach of X-ray structure-based drug design indicated as D-Phe-Pro dipeptide mimetics. The tetrahydroquinolyl sulfonamido de rivative Ig (LR-D/009) displayed the best inhibitory potency (IC50=0.0 18 mu m), with good selectivity over plasmin and trypsin. (C) 1997 Els evier Science Ltd.