Carbazolothiophene-2-carboxylic acid derivatives as endothelin receptor antagonists

被引：9

作者：

Babu, G

Yu, HM

Yang, SM

Fang, JM ^{[1
]}

机构：

[1] Natl Taiwan Univ, Dept Chem, Taipei 106, Taiwan

[2] Acad Sinica, Inst Biochem, Taipei 115, Taiwan

[3] Chiang Mai Univ, Dept Chem, Chiang Mai, Thailand

[4] Acad Sinica, Gen Res Ctr, Taipei 115, Taiwan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 05期

关键词：

coupling reactions; endothelin; samarium diiodide; thiophene; indole;

D O I：

10.1016/j.bmcl.2003.12.067

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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.

引用

收藏

页码：1129 / 1132

页数：4

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