BALANCED AT(1) AT(2) RECEPTOR ANTAGONISTS .4. XR510 AND RELATED 5-(3-AMIDOPROPANOYL)IMIDAZOLES POSSESSING EQUAL AFFINITY FOR THE AT(1) AND AT(2) RECEPTORS/

Authors
QUAN ML CHIU AT ELLIS CD WONG PC WEXLER RR TIMMERMANS PBMWM
Citation
Ml. Quan et al., BALANCED AT(1) AT(2) RECEPTOR ANTAGONISTS .4. XR510 AND RELATED 5-(3-AMIDOPROPANOYL)IMIDAZOLES POSSESSING EQUAL AFFINITY FOR THE AT(1) AND AT(2) RECEPTORS/, Journal of medicinal chemistry, 38(15), 1995, pp. 2938-2945
Citations number
34
Categorie Soggetti
Chemistry Medicinal
Journal title
Journal of medicinal chemistry → ACNP
ISSN journal
00222623
Volume
38
Issue
15
Year of publication
1995
Pages
2938 - 2945
Database
ISI
SICI code
0022-2623(1995)38:15<2938:BAARA.>2.0.ZU;2-0
Abstract
The identification of the AT(1) and AT(2) receptor subtypes has stimul ated interest in developing balanced angiotensin II receptor antagonis ts. A series of 5-(3-amidopropanoyl)imidazoles has been prepared which possess balanced affinity for the AT(1) and AT(2) receptors. XR510 (1 ), 1-[[2'-[[(isopentoxycarbonyl)amino]sulfonyl]-3- oro(1,1'-biphenyl)- 4-yl]methyl]-5-[3-(N-pyridin-3- tanamido)propanoyl]-4-ethyl-2-propyl-1 H-imidazole, potassium salt, exhibits subnanomolar affinity for both r eceptor sites. XR510 is very active in lowering blood pressure in rena l hypertensive rats and furosemide-treated dogs following oral adminis tration.