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Angiotensin converting enzyme inhibitors.
Pharmaceutisch Weekblad. Scientific Edition
|October 22, 1982
Summary
Angiotensin converting enzyme (ACE) inhibitors like captopril lower blood pressure in renovascular hypertension. New non-mercapto ACE inhibitors, such as enalapril, are being developed to reduce side effects and improve treatment.
Area of Science:
- Pharmacology
- Cardiovascular Medicine
- Medicinal Chemistry
Background:
- Renovascular hypertension is a condition where high blood pressure is caused by narrowed arteries to the kidneys.
- Inhibition of angiotensin converting enzyme (ACE) effectively lowers blood pressure in these patients.
- Captopril was an early orally active ACE inhibitor, but its side effects were linked to its thiol (SH) group.
Purpose of the Study:
- To describe the development of captopril and its analogues.
- To explore the structure-activity relationship of ACE inhibitors.
- To introduce novel non-mercapto ACE inhibitors derived from captopril to mitigate side effects.
Main Methods:
- Development of captopril as an orally active ACE inhibitor.
- Synthesis and evaluation of captopril analogues.
- Design and development of non-mercapto ACE inhibitors based on structural modifications.
Main Results:
- Captopril effectively lowers blood pressure in renovascular hypertension.
- The SH-group in captopril was associated with certain side effects.
- A series of non-mercapto ACE inhibitors were developed, showing potential for improved safety and efficacy.
Conclusions:
- ACE inhibition is a validated strategy for managing renovascular hypertension.
- Non-mercapto ACE inhibitors represent a significant advancement over earlier thiol-containing compounds.
- Enalapril, a potent and long-acting non-mercapto ACE inhibitor, shows promise in ongoing clinical trials.