• Corpus ID: 26193978

Personal and Historical Perspectives History of the Design of Captopril and Related Inhibitors of Angiotensin Converting Enzyme

  title={Personal and Historical Perspectives History of the Design of Captopril and Related Inhibitors of Angiotensin Converting Enzyme},
  author={David W. Cushman and Miguel A. Ondetti},
In describing the development of captopril and related antihypertensive drugs, we hope to resurrect a more specific meaning for the term "drug design," namely, the logical process whereby molecules are constructed for precise fit with a macromolecular receptor. Thus defined, drug design requires direct or indirect knowledge of the nature of the receptor, which in this case is the active center of a peptidase known historically as angiotensin converting enzyme (ACE). We believe that the… 

Beyond Carbon: The Contributions of South American Tropical Humid and Subhumid Forests to Ecosystem Services

Tropical forests are recognized for their role in providing diverse ecosystem services (ESs), with carbon uptake the best recognized. The capacity of tropical forests to provide ESs is strongly



Rational Design and Biochemical Utility of Specific Inhibitors of Angiotensin‐Converting Enzyme

The availability of structurally diverse ACE inhibitors with great potency and specificity provides a powerful biochemical tool for purification, localization, and characterization of ACE in different tissues, and for distinguishing related zinc metallopeptidases with similar properties.

Angiotensin-converting enzyme inhibitors: biochemical properties and biological actions.

The chemistry and biochemistry of angiotensin-converting enzyme inhibitors are reviewed with emphasis on data published since the publication of previous reviews, to give the reader an appreciation of the medical implications of this new type of antihypertensive agent.

Treatment of patients with severe hypertension by inhibition of angiotensin-converting enzyme.

It was found that haemodialysis or diuresis with frusemide enhanced the blood pressure response to the compound, and the presence of a measured low total blood volume was found to be associated with an exaggerated fall in blood pressure to a small dose of compound.

Conversion of Angiotensin I to Angiotensin II by Cell-free Extracts of Dog Lung

This communication describes some of the enzymes in extracts of dog lung that metabolize angiotensins I and II and particularly those catalysing the conversion ofAngiotensin I to angiotENSin II (“converting enzyme”) and the enzyme(s) responsible for the inactivation of ang Elliotensin II and angiotsin I are referred to as “destroying enzyme’.


  • W. Peart
  • Medicine
    Pharmacological reviews
  • 1965
Renin should refer purely to the enzyme extracted from the kidney, and the vast new field of renal, adrenal and cardiovascular physiology that this discovery opened up.

An angiotensin converting-enzyme inhibitor to identify and treat vasoconstrictor and volume factors in hypertensive patients.

Abstract The antihypertensive action of nonapeptide competitive inhibitor of angiotensin-1-converting enzyme was evaluated in 13 hypertensive patients. In 12 a single injection (1 to 4 mg per kilog...


  • S. Ferreira
  • Biology, Chemistry
    British journal of pharmacology and chemotherapy
  • 1965
While determining whether dimercaprol could potentiate in situ the slowly reacting substances released by the venom of Bothrops when acting on the guinea-pig isolated ileum, it was found that the venom itself had a strong potentiating action upon the concentrations elicited by bradykinin.

Design of specific inhibitors of angiotensin-converting enzyme: new class of orally active antihypertensive agents.

A hypothetical model of the active site of angiotensin-converting enzyme, based on known chemical and kinetic properties of the enzyme, has enabled a new class of potent and specific inhibitors, carboxyalkanoyl and mercaptoalkanoysl derivatives of proline, to be designed.