Vancomycin disulfide derivatives as antibacterial agents

A series of lipidated vancomycin analogues 1 bearing disulfide bonds within their lipid chains was designed and synthesized to optimize their ADME profiles while retaining antibacterial potency. These compounds exhibited good activity against resistant organisms and low accumulation in tissues such...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-02, Vol.14 (3), p.735-738
Hauptverfasser:	Mu, YongQi, Nodwell, Matthew, Pace, John L., Shaw, Jeng-Pyng, Judice, J.Kevin
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Biological and medical sciences Disulfides - chemical synthesis Disulfides - pharmacology Drug Resistance, Microbial Gram-Positive Bacteria - drug effects Kidney - drug effects Lipid Metabolism Liver - drug effects Male Medical sciences Microbial Sensitivity Tests Molecular Structure Pharmacology. Drug treatments Rats Rats, Sprague-Dawley Structure-Activity Relationship Vancomycin - analogs & derivatives Vancomycin - chemical synthesis Vancomycin - pharmacology Vancomycin Resistance
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Beschreibung
Zusammenfassung:	A series of lipidated vancomycin analogues 1 bearing disulfide bonds within their lipid chains was designed and synthesized to optimize their ADME profiles while retaining antibacterial potency. These compounds exhibited good activity against resistant organisms and low accumulation in tissues such as kidney and liver. The synthesis and biological activity of vancomycin disulfide derivatives are reported.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2003.11.040