New Semisynthetic Glycopeptides MDL 63,246 and MDL 63,042, and Other Amide Derivatives of Antibiotic A-40,926 Active against Highly Glycopeptide-resistant VanA Enterococci
| Autor: | Bianca Patrizia Andreini, Adriano Malabarba, Pietro Ferrari, Michael Kurz, Roberto Scotti, Beth P. Goldstein, Romeo Ciabatti, Maurizio Denaro |
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| Rok vydání: | 1995 |
| Předmět: |
Magnetic Resonance Spectroscopy
Stereochemistry medicine.drug_class Antibiotics Microbial Sensitivity Tests Enterococcus faecalis Microbiology Structure-Activity Relationship Vancomycin Drug Discovery medicine Chromatography High Pressure Liquid Pharmacology Molecular Structure biology Teicoplanin Drug Resistance Microbial Biological activity biochemical phenomena metabolism and nutrition biology.organism_classification Streptococcaceae Glycopeptide Anti-Bacterial Agents Enterococcus medicine.drug |
| Zdroj: | The Journal of Antibiotics. 48:869-883 |
| ISSN: | 1881-1469 0021-8820 |
| DOI: | 10.7164/antibiotics.48.869 |
| Popis: | A series of amide derivatives of natural glycopeptide A-40,926 (A), its 6B-methyl ester (MA) and 6B-decarboxy-6B-hydroxymethyl derivative (RA) were prepared with the aim of obtaining activity against glycopeptide-resistant enterococci. These compounds are structurally related to a class of amides of 34-de(acetylglucosaminyl)-34-deoxy teicoplanin which showed interesting activity against strains of Enterococcus faecalis and E. faecium highly resistant to both vancomycin and teicoplanin. Among them, RA-amides MDL 63,246 and MDL 63,042 were the most active derivatives against several Gram-positive bacteria, including VanB and VanC enterococci, and were moderately active (MIC range 0.5 approximately 64 micrograms/ml) against strains of Enterococcus for which vancomycin and teicoplanin MICs were > or = 128 micrograms/ml. The chemical rationale and the synthesis of these new series of glycopeptide derivatives are described. Preliminary in vitro data are reported and structure-activity relationships are discussed. |
| Databáze: | OpenAIRE |
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