BALANCED AT(1) AND AT(2) ANGIOTENSIN-II ANTAGONISTS .1. NEW ORALLY-ACTIVE 5-CARBOXYL IMIDAZOLYL BIPHENYL SULFONYLUREAS

Authors
DEPREZ P HECKMANN B CORBIER A VEVERT JP FORTIN M GUILLAUME J
Citation
P. Deprez et al., BALANCED AT(1) AND AT(2) ANGIOTENSIN-II ANTAGONISTS .1. NEW ORALLY-ACTIVE 5-CARBOXYL IMIDAZOLYL BIPHENYL SULFONYLUREAS, Bioorganic & medicinal chemistry letters, 5(22), 1995, pp. 2605-2610
Citations number
21
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
22
Year of publication
1995
Pages
2605 - 2610
Database
ISI
SICI code
0960-894X(1995)5:22<2605:BAAAAA>2.0.ZU;2-1
Abstract
A series of substituted imidazolyl biphenyl sulfonylureas have been sy nthesized. Substitution on the imidazole ring but essentially on the u rea side chain significantly increased AT(2) binding with cyclohexylme thyl, cyclopentylmethyl and benzyl as the most effective substituents. Imidazole 13d, as a representative member of this series, displayed n anomolar binding affinity for both the AT(1) and AT(2) angiotensin II receptor subtypes as well as oral activity.