ALPHA-PHENOXYPHENYLACETIC ACID-DERIVED ANGIOTENSIN-II ANTAGONISTS WITH LOW NANOMOLAR AT(1) AT(2) RECEPTOR SUBTYPE AFFINITY .2./

Authors
WALSH TF KIVLIGHN SD ZINGARO GJ FITCH KJ CHANG RSL FAUST KA CHEN TB LOTTI VJ SIEGL PKS PATCHETT AA GREENLEE WJ
Citation
Tf. Walsh et al., ALPHA-PHENOXYPHENYLACETIC ACID-DERIVED ANGIOTENSIN-II ANTAGONISTS WITH LOW NANOMOLAR AT(1) AT(2) RECEPTOR SUBTYPE AFFINITY .2./, Bioorganic & medicinal chemistry letters, 5(11), 1995, pp. 1151-1154
Citations number
9
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
11
Year of publication
1995
Pages
1151 - 1154
Database
ISI
SICI code
0960-894X(1995)5:11<1151:AAAAW>2.0.ZU;2-O
Abstract
Directed synthesis and pharmacological evaluation in a recently descri bed class of alpha-phenoxyphenylacetic acid bearing angiotensin II (AI I) receptor antagonists has afforded further potent AT(1)-selective AI I antagonists. Substitution in the central aromatic ring significantly increases AT(2) receptor affinity such that the n-propyl derivative 7 g displayed low nanomolar potency at both AT(1) and AT(2) receptor sub types.