Multivalent Antibiotics via Metal Complexes:  Potent Divalent Vancomycins against Vancomycin-Resistant Enterococci

Dimers of vancomycin (Van), linked by a rigid metal complex, [Pt(en)(H2O)2]2+, exhibit potent activities (MIC ∼0.8 μg/mL, ∼720 times more potent than that of Van itself) against vancomycin-resistant enterococci (VRE). The result suggests that combining metal complexation and receptor/ligand interact...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2003-11, Vol.46 (23), p.4904-4909
Main Authors: Xing, Bengang, Yu, Chun-Wing, Ho, Pak-Leung, Chow, Kin-Hung, Cheung, Terence, Gu, Hongwei, Cai, Zongwei, Xu, Bing
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - pharmacology
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Dimerization
Enterococcus - drug effects
Magnetic Resonance Spectroscopy
Medical sciences
Microbial Sensitivity Tests
Models, Molecular
Molecular Conformation
Organoplatinum Compounds - chemical synthesis
Organoplatinum Compounds - pharmacology
Pharmacology. Drug treatments
Spectrometry, Mass, Electrospray Ionization
Structure-Activity Relationship
Thermodynamics
Vancomycin - analogs & derivatives
Vancomycin - chemical synthesis
Vancomycin - pharmacology
Vancomycin Resistance
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Summary:Dimers of vancomycin (Van), linked by a rigid metal complex, [Pt(en)(H2O)2]2+, exhibit potent activities (MIC ∼0.8 μg/mL, ∼720 times more potent than that of Van itself) against vancomycin-resistant enterococci (VRE). The result suggests that combining metal complexation and receptor/ligand interaction offers a useful method to construct multivalent inhibitors.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm030417q