BALANCED ANGIOTENSIN-II RECEPTOR ANTAGONISTS .2. 4-AMINOMETHYLIMIDAZOLES AND ACYLAMINOMETHYLIMIDAZOLES

Authors
OLSON RE LIU J LALKA GK VANATTEN MK WEXLER RR CHIU AT NGUYEN TT MCCALL DE WONG PC TIMMERMANS PBMWM
Citation
Re. Olson et al., BALANCED ANGIOTENSIN-II RECEPTOR ANTAGONISTS .2. 4-AMINOMETHYLIMIDAZOLES AND ACYLAMINOMETHYLIMIDAZOLES, Bioorganic & medicinal chemistry letters, 4(18), 1994, pp. 2229-2234
Citations number
26
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
18
Year of publication
1994
Pages
2229 - 2234
Database
ISI
SICI code
0960-894X(1994)4:18<2229:BARA.4>2.0.ZU;2-T
Abstract
The introduction of aminomethyl and acylaminometyl substituents at the imidazole 4-position of 1- biphenylmethylimidazole-5-carboxylates imp arts affinity for the AT(2) receptor. The highest affinity was found w ith the 4-(2-pyridyl)-piperazin-l-ylmethyl group and the use of hexano ylsulfonamide as a tetrazole replacement, which led to XM953 (18d), wi th an AT(2) IC50 of 20 nM and an AT(2)/AT(1) IC50 ratio of 3.