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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