NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - THE DISCOVERY OF DMP-581 AND DMP-811

Authors
CARINI DJ ARDECKY RJ ENSINGER CL PRUITT JR WEXLER RR WONG PC HUANG SM AUNGST BJ TIMMERMANS PBMWM
Citation
Dj. Carini et al., NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - THE DISCOVERY OF DMP-581 AND DMP-811, Bioorganic & medicinal chemistry letters, 4(1), 1994, pp. 63-68
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
1
Year of publication
1994
Pages
63 - 68
Database
ISI
SICI code
0960-894X(1994)4:1<63:NARA-T>2.0.ZU;2-2
Abstract
A novel series of 4-alkylimidazoles have been prepared. Two of these c ompounds, DMP 581, 4-ethyl-2-propyl-1-[[2'-(1 l)biphenyl-4-yl]methyl]i midazole-5-carboxaldehyde, and DMP 811, l-5-yl)biphenyl-4-yl]methyl]im idazole-5-carboxylic acid, possess among the highes oral antihypertens ive potencieso acid, possess among the highest oral antihypertensive p otencies yet described for an angiotensin II antagonist. In addition, prodrugs of DMP 811 have been developed to further enhance the oral bi oavailability of the parent diacid.