EVALUATION OF HETEROCYCLIC ACID EQUIVALENTS AS TETRAZOLE REPLACEMENTSIN IMIDAZOPYRIDINE-BASED NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS

Authors
KIM D MANTLO NB CHANG RSL KIVLIGHN SD GREENLEE WJ
Citation
D. Kim et al., EVALUATION OF HETEROCYCLIC ACID EQUIVALENTS AS TETRAZOLE REPLACEMENTSIN IMIDAZOPYRIDINE-BASED NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 4(1), 1994, pp. 41-44
Citations number
11
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
41 - 44
Database
ISI
SICI code
0960-894X(1994)4:1<41:EOHAEA>2.0.ZU;2-T
Abstract
A series of imidazo[4,5-b]pyridine-based AII antagonists incorporating heterocyclic acid equivalents, e.g., oxathiadiazoles, thiatriazoles, and dioxobenzothiadiazines, are exemplified as novel non-peptide AII r eceptor antagonists. The most potent antagonist in this series, L-161, 177 (IC50 = 0.7 nM, rabbit aorta), bearing the oxathiadiazole, exhibit ed excellent in vivo profile after both iv and oral administration to conscious rats.