CGS 27830, a potent nonpeptide endothelin receptor antagonist
Autor: | Kenneth E. Lipson, Ben Mugrage, Randy L. Webb, John Moliterni, Suraj S. Shetty, Robert Neale, Leslie Anne Robinson, Catherine L. Cioffi, Michael H. Chin |
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Rok vydání: | 1993 |
Předmět: |
chemistry.chemical_classification
Stereochemistry Chemistry Endothelin receptor antagonist Carboxylic acid Organic Chemistry Clinical Biochemistry Dihydropyridine Antagonist Pharmaceutical Science Biological activity Biochemistry Chemical synthesis Competitive antagonist Drug Discovery medicine Molecular Medicine Endothelin receptor Molecular Biology medicine.drug |
Zdroj: | Bioorganic & Medicinal Chemistry Letters. 3:2099-2104 |
ISSN: | 0960-894X |
DOI: | 10.1016/s0960-894x(01)81025-8 |
Popis: | Treatment of the dihydropyridine carboxylic acid 1 with EDCI produced a diastereomeric mixture of chemically stable anhydrides. The meso-isomer, CGS 27830, was isolated by crystallization and found to be a potent (16 nM) endothelin receptor antagonist for the ETA receptor subtype. |
Databáze: | OpenAIRE |
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