Standard Article

Angiotensin-Converting Enzyme Inhibitors

Cardiovascular, Endocrine and Metabolic Diseases

  1. Edward W. Petrillo

Published Online: 15 SEP 2010

DOI: 10.1002/0471266949.bmc174

Burger's Medicinal Chemistry and Drug Discovery

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.

Author Information

  1. Pennington, NJ

Publication History

  1. 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.


  • antihypertensive;
  • congestive heart failure;
  • enzyme inhibitor;
  • peptide;
  • reninangiotensin system