Carbazolothiophene-2-carboxylic acid derivatives as endothelin receptor antagonists

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:14

Article

Babu, G ; Yu, HM ; Yang, SM ; Fang, JM

关键词: coupling reactions;    endothelin;    samarium diiodide;    thiophene;    indole;   

DOI  :  10.1016/j.bmcl.2003.12.067

来源: Elsevier

【 摘 要 】

The SmI2-promoted three-component coupling reaction of thiophene-2-carboxylate, indole-2-carbaldehyde and acetophenone provides an expedient route to a series of tetracyclic carbazolothiophene compounds bearing the indole and 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. (C) 2003 Elsevier Ltd. All rights reserved.

【 授权许可】

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