BALANCED AT(1) AND AT(2) ANGIOTENSIN-II ANTAGONISTS .2. POTENT 5-ALPHA-HYDROXYACID IMIDAZOLYL BIPHENYL SULFONYLUREAS

Authors
DEPREZ P GUILLAUME J CORBIER A FORTIN M VEVERT JP HECKMANN B
Citation
P. Deprez et al., BALANCED AT(1) AND AT(2) ANGIOTENSIN-II ANTAGONISTS .2. POTENT 5-ALPHA-HYDROXYACID IMIDAZOLYL BIPHENYL SULFONYLUREAS, Bioorganic & medicinal chemistry letters, 5(22), 1995, pp. 2611-2616
Citations number
18
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
2611 - 2616
Database
ISI
SICI code
0960-894X(1995)5:22<2611:BAAAAA>2.0.ZU;2-2
Abstract
Introduction of an alpha-hydroxyacid moiety in position 5 of the imida zole ring within the imidazolyl biphenyl sulfonyl urea series signific antly increased AT(2) binding. Structure activity relationship around this moiety is described and gave rise to balanced AII inhibitors with nanomolar affinity on both AT(1) and AT(2) receptors and with an AT(2 )/AT(1) ratio of between 0.4 and 3.