Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 40, Issue 8, Pages 798-804Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2005.01.011
Keywords
vancomycin; poly (ethylene glycol); anti-microbial activity
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PEG-amide vancomycin derivatives (V-3 position) have been synthesized and found to behave as prodrugs in vivo. demonstrating antimicrobial activity in mice when challenged with Staphylococcus aureus. The corresponding PEG-carbamate derivative,. do not manifest this in vivo activity, although both classes of compounds have similar in vitro rat plasma stability, Thus, it appears that extra vascular cleavage of the amide bond can occur if the condition of extended circulation of the conjugate is met, resulting in the release of vancolmycin. (c) 2005 Elsevier SAS. All rights reserved.
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