α-Phenoxyphenylacetic acid derived angiotensin II antagonists with low nanomolar AT1/AT2 receptor subtype affinity (Part II)

Autor: Peter K. S. Siegl, Salah D. Kivlighn, Gloria J. Zingaro, Tsing-Bau Chen, Kristie A. Faust, Victor J. Lotti, William J. Greenlee, Arthur A. Patchett, Thomas F. Walsh, Kenneth J. Fitch, Raymond S.L. Chang
Rok vydání: 1995
Předmět:
Zdroj: Bioorganic & Medicinal Chemistry Letters. 5:1151-1154
ISSN: 0960-894X
DOI: 10.1016/0960-894x(95)00185-v
Popis: Directed synthesis and pharmacological evaluation in a recently described class of α-phenoxyphenylacetic acid bearing angiotensin II (AII) receptor antagonists has afforded further potent AT 1 -selective AII antagonists. Substitution in the central aromatic ring significantly increases AT 2 receptor affinity such that the n -propyl derivative 7g displayed low nanomolar potency at both AT 1 and AT 2 receptor subtypes.
Databáze: OpenAIRE