咔唑并噻吩-2-羧酸衍生物作为内皮素受体拮抗剂
Carbazolothiophene-2-carboxylic acid derivatives as endothelin receptor antagonists.
作者信息
Babu Govindarajulu, Yu Hui-Ming, Yang Shyh-Ming, Fang Jim-Min
机构信息
Department of Chemistry, National Taiwan University, Taipei 106, Taiwan.
出版信息
Bioorg Med Chem Lett. 2004 Mar 8;14(5):1129-32. doi: 10.1016/j.bmcl.2003.12.067.
The SmI(2)-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.
二碘化钐促进的噻吩 - 2 - 羧酸盐、吲哚 - 2 - 甲醛和苯乙酮的三组分偶联反应为一系列带有吲哚环和噻吩环的四环咔唑并噻吩化合物提供了一条便捷的合成路线。在这些样品中，9 - 苄基 - 4 - 甲基 - 4 - (4 - 羟基苯基) - 10 - 氧代 - 4,10 - 二氢咔唑并[2,3 - b]噻吩 - 2 - 羧酸（18）对内皮素 - 1诱导的细胞内钙离子浓度升高表现出最强的抑制作用。
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