Lipophilic vancomycin aglycon dimer with high activity against vancomycin-resistant bacteria
| Autor: | Jayanta Haldar, Venkateswarlu Yarlagadda, Paramita Sarkar, Goutham B. Manjunath |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
Stereochemistry
Dimer Clinical Biochemistry Pharmaceutical Science Microbial Sensitivity Tests Biochemistry chemistry.chemical_compound Vancomycin Drug Resistance Bacterial Drug Discovery medicine Moiety Molecular Biology Bacteria biology Organic Chemistry Biological activity biochemical phenomena metabolism and nutrition biology.organism_classification Lipids Anti-Bacterial Agents Solubility chemistry Doxorubicin Molecular Medicine Peptidoglycan Antibacterial activity Dimerization Linker medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 25:5477-5480 |
| ISSN: | 0960-894X |
| Popis: | Antibiotic-resistant superbugs such as vancomycin-resistant Enterococci (VRE) and Staphylococci have become a major global health hazard. To address this issue, we synthesized vancomycin aglycon dimers to systematically probe the impact of a linker on biological activity. A dimer having a pendant lipophilic moiety in the linker showed ∼300-fold more activity than vancomycin against VRE. The high activity of the compound is attributed to its enhanced binding affinity to target peptides which resulted in improved peptidoglycan (cell wall) biosynthesis inhibition. Therefore, our studies suggest that these compounds, prepared by using facile synthetic methodology, can be used to combat vancomycin-resistant bacterial infections. |
| Databáze: | OpenAIRE |
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