Angiotensin-Converting Enzyme Inhibitors
Cardiovascular, Endocrine and Metabolic Diseases
Published Online: 15 SEP 2010
Copyright © 2003 by John Wiley & Sons, Inc. All rights reserved.
Burger's Medicinal Chemistry and Drug Discovery
How to Cite
Petrillo, E. W. 2010. Angiotensin-Converting Enzyme Inhibitors. Burger's Medicinal Chemistry and Drug Discovery. 267–302.
- Published Online: 15 SEP 2010
The discovery of captopril, the first orally active angiotensin-converting enzyme inhibitor, showed that blockade of the renin-angiotensin system effectively lowers blood pressure in a wide spectrum of patients with hypertension. Captopril was designed using a hypothetical model of the enzyme active site that subsequently guided the design of new classes of inhibitors. Because ACE inhibitors retard the progression of cardiovascular disease and the complications of diabetes, leading to an overall reduction in mortality, they have become one of the most widely used drug classes in cardiovascular medicine. New genetic and structural evidence has revealed that ACE has two functional catalytic domains with differences that may be exploited in the future to design inhibitors with superior properties.
- congestive heart failure;
- enzyme inhibitor;
- reninangiotensin system