Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors

…, HW Hamilton, MD Taylor, MJ Ryan…

Index: Patt, William C.; Hamilton, Harriet W.; Taylor, Michael D.; Ryan, Michael J.; Taylor, David G.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 14 p. 2562 - 2572

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Citation Number: 298

Abstract

A series of renin inhibitors was synthesized that contained a 2-amino-4-thiazolyl moiety at the Pz position. These derivatives are potent inhibitore 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 ...