BALANCED AT(1) AND AT(2) ANGIOTENSIN-II ANTAGONISTS .3. POTENT AND ORALLY-ACTIVE 5-BETA-KETOSULFOXIDE IMIDAZOLYL BIPHENYL SULFONYLUREAS

Authors
DEPREZ P GUILLAUME J CORBIER A VEVERT JP FORTIN M HECKMANN B
Citation
P. Deprez et al., BALANCED AT(1) AND AT(2) ANGIOTENSIN-II ANTAGONISTS .3. POTENT AND ORALLY-ACTIVE 5-BETA-KETOSULFOXIDE IMIDAZOLYL BIPHENYL SULFONYLUREAS, Bioorganic & medicinal chemistry letters, 5(22), 1995, pp. 2617-2622
Citations number
20
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
2617 - 2622
Database
ISI
SICI code
0960-894X(1995)5:22<2617:BAAAAA>2.0.ZU;2-X
Abstract
In the imidazolyl biphenyl sulfonylurea series, effects of substitutio n in position 5 of the imidazole ring with enolic ketone moiety were s tudied on AT(2) binding. beta-ketosulfoxide, beta-ketosulfone and beta -ketoester proved to be highly effective substituents for potent nanom olar binding affinity on both AT(1) and AT(2) receptor subtypes. This led to the identification of beta-ketophenylsulfoxide RU 64276 as a po tent and orally active AT(1) antagonist and AT(2) binding inhibitor.