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Title: Design and Optimization of Renin Inhibitors: Orally Bioavailable Alkyl Amines

Journal Article · · Bioorganic and Medicinal Chemistry Letters

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{sub 50} of 0.47 nM, caused a sustained reduction in mean arterial blood pressure in a double transgenic rat model of hypertension.

Research Organization:
Brookhaven National Lab. (BNL), Upton, NY (United States). National Synchrotron Light Source
Sponsoring Organization:
Doe - Office Of Science
DOE Contract Number:
DE-AC02-98CH10886
OSTI ID:
980136
Report Number(s):
BNL-93054-2010-JA; TRN: US201015%%1521
Journal Information:
Bioorganic and Medicinal Chemistry Letters, Vol. 19, Issue 13; ISSN 0968-0896
Country of Publication:
United States
Language:
English