Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists

Authors
Ahn, HS Arik, L Boykow, G Burnett, DA Caplen, MA Czarniecki, M Domalski, MS Foster, C Manna, M Stamford, AW Wu, YS
Citation
Hs. Ahn et al., Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists, BIOORG MED, 9(14), 1999, pp. 2073-2078
Citations number
14
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
14
Year of publication
1999
Pages
2073 - 2078
Database
ISI
SICI code
0960-894X(19990719)9:14<2073:SROPAT>2.0.ZU;2-V
Abstract
A series of pyrroloquinazolines has been discovered that represent novel sm all molecule inhibitors of the intramolecular ligand of the thrombin recept or. Analogs were prepared to study the structure-activity relationships of substitution at the N1, N3, and N7 positions of the heterocycle. Compounds 4e and 4f have been identified with IC50's of 56 and 52 nM, respectively. ( C) 1999 Elsevier Science Ltd. All rights reserved.