Carbazolothiophene-2-carboxylic acid derivatives as endothelin receptor antagonists |
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Authors: | Babu Govindarajulu Yu Hui-Ming Yang Shyh-Ming Fang Jim-Min |
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Institution: | Department of Chemistry, National Taiwan University, Taipei 106, Taiwan. |
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Abstract: | 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-dihydrocarbazolo2,3-b]thiophene-2-carboxylic acid (18) shows the most potent inhibition against the endothelin-1 induced increase of intracellular calcium ion concentration. |
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