Design, synthesis and biological evaluation of berberine-benzimidazole hybrids as new type of potentially DNA-targeting antimicrobial agents.

摘要: Abstract A series of novel berberine-benzimidazole derivatives were conveniently and efficiently synthesized characterized by NMR, IR, MS HRMS spectra. Most the prepared compounds showed effective antimicrobial activities in contrast with clinical norfloxacin, chloromycin fluconazole. Especially, compound 5d exhibited good anti-MRSA, anti- Escherichia coli, Salmonella typhi activity low MIC values 2–8 μg/mL, which comparable or even superior to reference drugs. The preliminarily interactive investigation revealed that most active could effectively intercalate into DNA form -DNA complex cleavage agarose gel electrophoresis experiments. It was also found able permeabilize membranes both Gram-positive (MRSA) Gram-negative ( E . coli DH52) bacteria. Experiments molecular docking human serum albumin (HSA) transport hydrophobic interactions hydrogen bonds play important roles association HSA.