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Optimization of the central linker of dicationic bis-benzimidazole anti-MRSA and anti-VRE agents
Authors:Laixing Hu  Maureen L. Kully  David W. Boykin  Norman Abood
Affiliation:1. Department of Chemistry, Georgia State University, Atlanta, GA 30303-3083, USA;2. Naeja Pharmaceutical Inc., Edmonton, Alta., Canada T6E 5V2;3. Immtech Inc. 150 Fairway Suite 150, Vernon Hills, IL 60061-1860, USA
Abstract:A series of bis-benzimidazole diamidine compounds containing different central linkers has been synthesized and evaluated for in vitro antibacterial activities, including drug-resistant bacterial strains. Seven compounds have shown potent antibacterial activities. The anti-MRSA and anti-VRE activities of compound 1h were more potent than that of the lead compound 1a and vancomycin.
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