Carbazolothiophene-2-carboxylic acid derivatives as endothelin receptor antagonists
| Autor: | Shyh-Ming Yang, Govindarajulu Babu, Jim-Min Fang, Hui-Ming Yu |
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| Rok vydání: | 2004 |
| Předmět: |
Endothelin Receptor Antagonists
Stereochemistry Carboxylic acid Clinical Biochemistry Carbazoles Carboxylic Acids Pharmaceutical Science chemistry.chemical_element CHO Cells Thiophenes Calcium Medicinal chemistry Biochemistry Chemical synthesis Coupling reaction chemistry.chemical_compound Cricetinae Drug Discovery Thiophene Animals Molecular Biology Indole test chemistry.chemical_classification Chemistry Organic Chemistry General Medicine Thiophene derivatives Endothelin 1 Rats Intracellular calcium ion Molecular Medicine Endothelin receptor Acetophenone |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 14:1129-1132 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2003.12.067 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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