Discovery of novel berberine imidazoles as safe antimicrobial agents by down regulating ROS generation.
作者： Si-Qi Wen , Ponmani Jeyakkumar , Srinivasa Rao Avula , Ling Zhang , Cheng-He Zhou
DOI: 10.1016/J.BMCL.2016.04.070
关键词:
摘要: A series of novel berberine-based imidazole derivatives as new type antimicrobial agents were developed and characterized. Most them gave good antibacterial activity toward the Gram-positive negative bacteria. Noticeably, imidazolyl berberine 3a exhibited low MIC value 1μg/mL against Eberthella typhosa, which was even superior to reference drugs berberine, chloromycin norfloxacin. The cell toxicity ROS generation assay indicated that compound showed toxicity. interactive investigation by UV-vis spectroscopic method revealed could effectively intercalate into calf thymus DNA form 3a-DNA complex might further block replication exert powerful activities. binding behavior topoisomerase IB hydrogen bonds electrostatic interactions played important roles in association with IB.
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