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.