Multivalent antibiotics via metal complexes: potent divalent vancomycins against vancomycin-resistant enterococci.
Dimers of vancomycin (Van), linked by a rigid metal complex, [Pt(en)(H(2)O)(2)](2+), exhibit potent activities (MIC approximately 0.8 mug/mL, approximately 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.
Xing
Bengang
B
Department of Chemistry, The Hong Kong University of Science and Technology, Clear Water Bay, Hong Kong, China.
Yu
Chun-Wing
CW
Ho
Pak-Leung
PL
Chow
Kin-Hung
KH
Cheung
Terence
T
Gu
Hongwei
H
Cai
Zongwei
Z
Xu
Bing
B
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D019281:Dimerization; D016983:Enterococcus / Q000187:drug effects*; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D008968:Molecular Conformation; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D021241:Spectrometry, Mass, Electrospray Ionization; D013329:Structure-Activity Relationship; D013816:Thermodynamics; D014640:Vancomycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D020713:Vancomycin Resistance
D000900:Anti-Bacterial Agents; D009944:Organoplatinum Compounds; C479681:diaqua(ethylenediamine)platinum(II); D014640:Vancomycin