BALANCED ANGIOTENSIN-II RECEPTOR ANTAGONISTS .1. THE EFFECTS OF BIPHENYL ORTHO SUBSTITUTION ON AT(1) AT(2) AFFINITIES/

Authors
QUAN ML OLSON RE CARINI DJ ELLIS CD HILLYER GL LALKA GK LIU J VANATTEN MK CHIU AT WONG PC WEXLER RR TIMMERMANS PBMWM
Citation
Ml. Quan et al., BALANCED ANGIOTENSIN-II RECEPTOR ANTAGONISTS .1. THE EFFECTS OF BIPHENYL ORTHO SUBSTITUTION ON AT(1) AT(2) AFFINITIES/, Bioorganic & medicinal chemistry letters, 4(16), 1994, pp. 2011-2016
Citations number
25
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
16
Year of publication
1994
Pages
2011 - 2016
Database
ISI
SICI code
0960-894X(1994)4:16<2011:BARA.T>2.0.ZU;2-A
Abstract
Biphenyl ''ortho''-substitution of DuP 753-like AT(1)-selective angiot ensin II receptor antagonists provides AT(2) affinity. When combined w ith a sulfonylcarbamate as the acid isostere, balanced AT(1)/AT(2) rec eptor antagonists were obtained. Some compounds exhibited nanomolar af finities for both receptors and good AT(2)/AT(1) ratios; these compoun ds also produce potent and prolonged antihypertensive effects in renal hypertensive rats.