Design and Optimization of Renin Inhibitors: Orally Bioavailable Alkyl Amines

Journal Article · Wed Dec 31 23:00:00 EST 2008 · Bioorganic and Medicinal Chemistry Letters

DOI:https://doi.org/10.1016/j.bmcl.2009.04.140· OSTI ID:980136

Tice, C; Xu, Z; Yuan, J; Simpson, R; Cacatian, S; Flaherty, P; Zhao, W; Guo, J

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

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
99 GENERAL AND MISCELLANEOUS
AMINES
BLOOD PRESSURE
DESIGN
DRUGS
HYPERTENSION
LEAD COMPOUNDS
OPTIMIZATION
ORAL ADMINISTRATION
RATS
REDUCTION
RENIN
national synchrotron light source