DESIGN, SYNTHESIS AND IN-VITRO ACTIVITIES OF A SERIES OF BENZIMIDAZOLE BENZOXAZOLE GLYCOPROTEIN IIB/IIIA INHIBITORS/

Authors
XUE CB RAFALSKI M RODERICK J EYERMANN CJ MOUSA S OLSON RE DEGRADO WF
Citation
Cb. Xue et al., DESIGN, SYNTHESIS AND IN-VITRO ACTIVITIES OF A SERIES OF BENZIMIDAZOLE BENZOXAZOLE GLYCOPROTEIN IIB/IIIA INHIBITORS/, Bioorganic & medicinal chemistry letters, 6(3), 1996, pp. 339-344
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
3
Year of publication
1996
Pages
339 - 344
Database
ISI
SICI code
0960-894X(1996)6:3<339:DSAIAO>2.0.ZU;2-S
Abstract
A potent centrally constrained series of benzimidazole and benzoxazole glycoprotein IIb/IIIa inhibitors has been discovered based on the sol ution conformation of a cyclic RGD-containing peptide, DMP 728. The hi gh potency of this series of compounds in the inhibition of platelet a ggregation requires a benzamidine as the basic moiety and an alpha-car bamate or sulfonamide substituted beta-alanine as the acidic moiety.