Synthesis and in vitro activity of dicationic bis-benzimidazoles as a new class of anti-MRSA and anti-VRE agents.
A new class of novel bis-benzimidazole diamidine compounds have been synthesized and evaluated for in vitro antibacterial activities, including drug-resistant bacterial strains. Anti-MRSA and anti-VRE activities of the most potent compound 1 were more active than Vancomycin. The mechanism of action for this class of compounds appears to be different from existing antibiotics. Bis-benzimidazole diamidine compounds have potential for further investigation as a new class of potent anti-MRSA and anti-VRE agents.
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 / Q000737:chemistry / Q000145:classification / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000145:classification / Q000494:pharmacology*; D024901:Drug Resistance, Multiple, Bacterial / Q000187:drug effects; D016984:Enterococcus faecium / Q000187:drug effects*; D016106:Methicillin Resistance / Q000187:drug effects; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship; D020713:Vancomycin Resistance / Q000187:drug effects
D000900:Anti-Bacterial Agents; D001562:Benzimidazoles; C009712:bis-benzimidazole