BENZOFURAN BASED ANGIOTENSIN-II ANTAGONISTS RELATED TO GR117289 .3. GR138950, A TRIFLAMIDE WITH HIGH ORAL BIOAVAILABILITY

Authors
DOWLE MD JUDD DB MIDDLEMISS D SCOPES DIC ROSS BC PASS M TRANQUILLINI E JACK TI HOBSON JE PANCHAL TA STUART PG DREW GM ROBERTSON MJ HILDITCH A CLARK KL TRAVERS A HUNT AAE MANCHEE GR WALKER DG EDDERSHAW PJ DONNELLY M BAYLISS MK
Citation
Md. Dowle et al., BENZOFURAN BASED ANGIOTENSIN-II ANTAGONISTS RELATED TO GR117289 .3. GR138950, A TRIFLAMIDE WITH HIGH ORAL BIOAVAILABILITY, Bioorganic & medicinal chemistry letters, 3(10), 1993, pp. 2047-2050
Citations number
5
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
10
Year of publication
1993
Pages
2047 - 2050
Database
ISI
SICI code
0960-894X(1993)3:10<2047:BBAART>2.0.ZU;2-1
Abstract
The identification of GR138950, a non-peptide antagonist of angiotensi n II with high oral bioavailability, is described. GR138950 is a poten t and selective ATI receptor antagonist which causes marked falls in b lood pressure in renal hypertensive rats after either systemic or oral administration. It has high bioavailability in both rats and dogs and has been selected as our second candidate for clinical development.