Fine Tuning of physico-chemical parameters to optimise a new series of novobiocin analogues
Autor: | Michel Murer, Michel Klich, Fabienne Chatreaux, Anne Ferreira, Véronique Loyau, Alain Bonnefoy, Laurent Schio, Pascale Mauvais |
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Rok vydání: | 2001 |
Předmět: |
Staphylococcus aureus
Clinical Biochemistry Substituent Pharmaceutical Science Microbial Sensitivity Tests Biochemistry chemistry.chemical_compound Coumarins Drug Discovery medicine Organic chemistry heterocyclic compounds Molecular Biology Novobiocin Antibacterial agent chemistry.chemical_classification Chemistry Aryl Organic Chemistry Combinatorial chemistry Anti-Bacterial Agents Dissociation constant Lipophilicity Molecular Medicine Antibacterial activity Lactone medicine.drug |
Zdroj: | Bioorganic & Medicinal Chemistry Letters. 11:1461-1464 |
ISSN: | 0960-894X |
DOI: | 10.1016/s0960-894x(01)00257-8 |
Popis: | A novel series of novobiocin analogues has been synthesised by removing the lipophilic aryl chain in novobiocin and introducing an amino substituent. The structural modifications have been dictated by the control of lipophilicity and the dissociation constant of the resulting compounds. Antibacterial activity of the new coumarin derivatives could be correlated with the amount of uncharged form in physiological conditions. |
Databáze: | OpenAIRE |
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