Carbazolothiophene-2-carboxylic acid derivatives as endothelin receptor antagonists
Resource
Bioorganic & Medicinal Chemistry Letters 14,1129-1132
Journal
Bioorganic & Medicinal Chemistry Letters 14
Pages
1129-1132
Date Issued
2004
Date
2004
Author(s)
DOI
246246/2006111501232963
Abstract
The SmI2-promoted three-component coupling reaction of thiophene-2-carboxylate, indole-2-carbaldehyde & acetophenone provides an expedient route to a series of tetracyclic carbazolothiophene compounds bearing the indole & thiophene rings. Among these samples, 9-benzyl-4-methyl-4-(4-hydroxyphenyl)-10-oxo-4,10-dihydrocarbazolo[2,3-b]thiophene-2-carboxylic acid (18) shows the most potent inhibition against the endothelin-1 induced increase of intracellular calcium ion concentration.
Subjects
Coupling reactions
Endothelin
Samarium diiodide
Thio-phene
Indole
SDGs
Type
journal article
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