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Endothelin receptor antagonists: structures, synthesis, selectivity and therapeutic applications
1Department of Medicinal Chemistry, Actelion Pharmaceuticals Ltd, Allschwil / BL, Switzerland. christoph.boss@actelion.com
Current Medicinal Chemistry
|February 28, 2002
Summary
Endothelin receptor antagonists are promising therapeutics for cardiovascular, cerebrovascular, and renal diseases. This review focuses on small organic molecules targeting endothelin receptors, detailing their synthesis and therapeutic potential.
Area of Science:
- Pharmacology
- Medicinal Chemistry
Background:
- Endothelin (ET) is a potent vasoconstrictor with three isoforms (ET-1 to ET-3).
- ET acts on two receptor subtypes: endothelin-A (ET(A)) and endothelin-B (ET(B)).
- Endothelin receptor antagonists are under clinical development for various diseases.
Purpose of the Study:
- To review small organic molecule endothelin receptor antagonists.
- To describe their synthesis, structure-activity relationships, and selectivity profiles.
- To discuss their potential therapeutic indications.
Main Methods:
- Literature review of endothelin receptor antagonists.
- Focus on small organic molecules suitable for oral administration.
- Analysis of synthesis, SAR, selectivity, and therapeutic applications.
Main Results:
- Multiple structural classes of small organic ET receptor antagonists have been developed.
- Detailed structure-activity relationships and receptor-subtype selectivity are presented.
- Potential applications in cardiovascular, cerebrovascular, and renal diseases are discussed.
Conclusions:
- Small organic molecules represent a significant class of endothelin receptor antagonists.
- These compounds show promise for treating various diseases.
- Further research into their synthesis and therapeutic applications is warranted.