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.
Export Options
About this article
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 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Subclinical Thyroid Dysfunction and Cardiovascular Outcomes among Prospective Cohort Studies
Endocrine, Metabolic & Immune Disorders - Drug Targets Properdin and Complement Activation: A Fresh Perspective
Current Drug Targets Microvascular Endothelial Dysfunction in Obesity and Hypertension
Current Pharmaceutical Design Past, Present and Future of Electroanalytical Sensor for Aspirin, Ibuprofen and Paracetamol Detection
Current Pharmaceutical Analysis Angiotensin II in the Human Physiology: Novel Ways for Synthetic Compounds Utilization
Current Medicinal Chemistry Vascular Wall Shear Stress in Clinical Practice
Current Vascular Pharmacology Src Inhibitors and Angiogenesis
Current Pharmaceutical Design Solification with Hydrobromic Acid as a Factor Defining the Antiarrhythmic Effect of Lappaconitine Derivatives
Letters in Drug Design & Discovery The Development of Floating Multiple Unit Mini Tablets of Bosentan Using QbD: Characterisation and Pharmacokinetic Study
Drug Delivery Letters Sphingomyelinase Inhibition Suggests a Possible New Strategy for the Treatment of Inflammatory Bowel Disease
Current Drug Therapy The DOCA-Salt Hypertensive Rat as a Model of Cardiovascular Oxidative and Inflammatory Stress
Current Cardiology Reviews Mechanosensitive Ion Channels as Drug Targets
Current Drug Targets - CNS & Neurological Disorders Endothelial Regenerative Capacity and Aging: Influence of Diet, Exercise and Obesity
Current Cardiology Reviews Therapeutic Approaches in the Stimulation of the Coronary Collateral Circulation
Current Cardiology Reviews Role of Secretory Phospholipase A2 in CNS Inflammation: Implications in Traumatic Spinal Cord Injury
CNS & Neurological Disorders - Drug Targets Neuroregeneration in Parkinson’s Disease: From Proteins to Small Molecules
Current Neuropharmacology Anticancer Mammalian Target of Rapamycin (mTOR) Signaling Pathway Inhibitors: Current Status, Challenges and Future Prospects in Management of Epilepsy
CNS & Neurological Disorders - Drug Targets Memantine and Kynurenic Acid: Current Neuropharmacological Aspects
Current Neuropharmacology Role of Perindopril in the Prevention of Stroke
Recent Patents on Cardiovascular Drug Discovery Impact of Pre-Diabetes and Diabetes on Cardiovascular Outcomes
Current Vascular Pharmacology