The preparation of zaragozic acid A analogues by directed biosynthesis
| Autor: | John G. MacConnell, Raymond F. White, Tom S. Chen, J. D. Bergstrom, L. Huang, Richard L. Monaghan, Georgette Dezeny, Brian R. Petuch, Lawrence F. Colwell, Byron H. Arison |
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| Rok vydání: | 1994 |
| Předmět: |
Pharmacology
Magnetic Resonance Spectroscopy ATP synthase biology Stereochemistry Chemistry Fungi Tricarboxylic Acids Zaragozic acid Bridged Bicyclo Compounds Heterocyclic In vitro Squalene chemistry.chemical_compound Bridged Bicyclo Compounds Farnesyl-Diphosphate Farnesyltransferase Biosynthesis Biochemistry Enzyme inhibitor Drug Discovery biology.protein Phenyl group Alkyl side chain |
| Zdroj: | The Journal of antibiotics. 47(11) |
| ISSN: | 0021-8820 |
| Popis: | Zaragozic acid A analogues are produced by an unidentified sterile fungus when it is exogenously supplied with 2-thiophenecarboxylic acid, 3-thiophenecarboxylic acid, 2-furoic acid, 2-fluorobenzoic acid, 3-fluorobenzoic acid, or 4-fluorobenzoic acid. The analogues carry 2-thiophenyl, 3-thiophenyl, 2-furyl, o-fluorophenyl, m-fluorophenyl, or p-fluorophenyl group, respectively, at C-6' of the C-1 alkyl side chain replacing the phenyl group of natural zaragozic acid A. All the new analogues of zaragozic acid A possess picomolar inhibitory activity against squalene synthase in vitro. |
| Databáze: | OpenAIRE |
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