Optimization of the central linker of dicationic bis-benzimidazole anti-MRSA and anti-VRE agents.
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.
Hu
Laixing
L
Department of Chemistry, Georgia State University, Atlanta, GA 30303-3083, USA.
Kully
Maureen L
ML
Boykin
David W
DW
Abood
Norman
N
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D002412:Cations / Q000737:chemistry; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D010419:Pentamidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D020713:Vancomycin Resistance / Q000187:drug effects*
D000900:Anti-Bacterial Agents; D001562:Benzimidazoles; D002412:Cations; C542838:bis-benzimidazole diamidine; C009712:bis-benzimidazole; D010419:Pentamidine