Potent triazolinone-based angiotensin II receptor antagonists with equivalent affinity for both the AT1 and AT2 subtypes

Autor: Ralph A. Rivero, Peter K. S. Siegl, K. L. Flanagan, Salah D. Kivlighn, Wallace T. Ashton, Gloria J. Zingaro, Tsing-Bau Chen, Victor J. Lotti, R. S. L. Chang, S. S. O'malley, W.J. Greenlee, Linda L. Chang
Rok vydání: 1994
Předmět:
Zdroj: Bioorganic & Medicinal Chemistry Letters. 4:2787-2792
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(01)80595-3
Popis: A series of subnanomolar (IC50 triazolinone-based AT1/AT2-balanced AII antagonists has been identified. The 70-240-fold gain in AT2 activity relative to prototype compounds was achieved by the introduction of a 5-acylamino group on the N2-aryl moiety and the addition of (3-F-5'-Pr)biphenyl substituents on 4. These analogues exhibited AT2/AT1 IC50 rations of ≤1 in multiple assay systems including human adrenal.
Databáze: OpenAIRE
načítá se...