Synthesis and biological evaluation of coumarincarboxylic acids as inhibitors of gyrase B. L-rhamnose as an effective substitute for L-noviose
| Autor: | Michel Klich, Claudine Dupuis-Hamelin, Jeannine Collard, Patrice Lassaigne, Pascale Mauvais, Didier Ferroud, Alain Bonnefoy, Branislav Musicki |
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| Rok vydání: | 1999 |
| Předmět: |
Rhamnose
Stereochemistry Carboxylic acid Clinical Biochemistry Carboxylic Acids Pharmaceutical Science Biochemistry Chemical synthesis DNA gyrase chemistry.chemical_compound Coumarins Drug Discovery Escherichia coli medicine Topoisomerase II Inhibitors Moiety heterocyclic compounds Enzyme Inhibitors Molecular Biology Novobiocin Antibacterial agent chemistry.chemical_classification Molecular Structure DNA Superhelical Organic Chemistry Glycoside Anti-Bacterial Agents chemistry DNA Gyrase Molecular Medicine medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 9:2881-2886 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(99)00493-x |
| Popis: | A series of novobiocin-like coumarincarboxylic acids has been prepared bearing the L-rhamnosyl moiety as the sugar portion of the molecule. The similar DNA gyrase inhibitory activity of the novel class of coumarins to that of novobiocin demonstrates that L-rhamnose can effectively replace L-noviose. Introduction of alkyl side-chains at C-5 of coumarin leads to improved in vitro antibacterial properties in the novel series. |
| Databáze: | OpenAIRE |
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