Design and Optimization of Renin Inhibitors: Orally Bioavailable Alkyl Amines

Abstract Structure-based drug design led to the identification of a novel class of potent, low MW alkylamine renin inhibitors. Oral administration of lead compound 21l , with MW of 508 and IC 50 of 0.47 nM, caused a sustained reduction in mean arterial blood pressure in a double transgenic rat model of hypertension.