Abstract
Endothelin (ET) was discovered in 1988 and is the most potent vasoconstrictive peptide known to date. It exists in three isoforms (ET-1 to ET-3) and acts on two endothelin receptor subtypes, the endothelin-A (ETA)-receptor and the endothelin-B (ETB)-receptor. Endothelin receptor antagonists are novel therapeutics in clinical development for different cardiovascular, cerebrovascular, and renal diseases. Several different structural classes of endothelin receptor antagonists have been discovered within the last decade, starting from peptidic- and peptidomimetic structures to small organic molecules suitable as therapeutics for oral administration. Focussing on the small organic molecules, the different structural classes of ET-receptor antagonists are described with respect to synthesis, structure-activity-relationships, receptor-subtype-selectivity profile, and where possible, intended therapeutic indications.
Keywords: Endothelin Receptor Antagonists, Sitaxsentan, Darusentan, Tezosentan, Myriceric Acid-Derivatives, Pyrrolidine-3-Carboxylic Acids, Tetra-Substituted Pyrimidine
Current Medicinal Chemistry
Title: Endothelin Receptor Antagonists: Structures, Synthesis, Selectivity and Therapeutic Applications
Volume: 9 Issue: 3
Author(s): C. Boss, M. Bolli and T. Weller
Affiliation:
Keywords: Endothelin Receptor Antagonists, Sitaxsentan, Darusentan, Tezosentan, Myriceric Acid-Derivatives, Pyrrolidine-3-Carboxylic Acids, Tetra-Substituted Pyrimidine
Abstract: Endothelin (ET) was discovered in 1988 and is the most potent vasoconstrictive peptide known to date. It exists in three isoforms (ET-1 to ET-3) and acts on two endothelin receptor subtypes, the endothelin-A (ETA)-receptor and the endothelin-B (ETB)-receptor. Endothelin receptor antagonists are novel therapeutics in clinical development for different cardiovascular, cerebrovascular, and renal diseases. Several different structural classes of endothelin receptor antagonists have been discovered within the last decade, starting from peptidic- and peptidomimetic structures to small organic molecules suitable as therapeutics for oral administration. Focussing on the small organic molecules, the different structural classes of ET-receptor antagonists are described with respect to synthesis, structure-activity-relationships, receptor-subtype-selectivity profile, and where possible, intended therapeutic indications.
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Cite this article as:
Boss C., Bolli M. and Weller T., Endothelin Receptor Antagonists: Structures, Synthesis, Selectivity and Therapeutic Applications, Current Medicinal Chemistry 2002; 9 (3) . https://dx.doi.org/10.2174/0929867023371139
DOI https://dx.doi.org/10.2174/0929867023371139 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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