Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors.
Basic Information
ID: ALA1125476
Journal: J Med Chem
Title: Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors.
Authors: Patt WC, Hamilton HW, Taylor MD, Ryan MJ, Taylor DG, Connolly CJ, Doherty AM, Klutchko SR, Sircar I, Steinbaugh BA.
Abstract: A series of renin inhibitors was synthesized that contained a 2-amino-4-thiazolyl moiety at the P2 position. These derivatives are potent inhibitors of monkey renin in vitro and are selective in that they only weakly inhibit the closely related aspartic proteinase, bovine cathepsin D. Four compounds exhibited oral blood pressure lowering activity in high-renin normotensive monkeys. One of these compounds, 22 (PD 134672), was selected for further evaluation in renal hypertensive monkeys, on the basis of its superior efficacy and duration of action in the in vitro assays and the normotensive primate model.
CiteXplore: 1635057
DOI: 10.1021/jm00092a006
Patent ID: ┄