Hydrophobic modification Thr of polymyxin E: Effect on activity and toxicity

Chengcheng Tang, Yiran Song,Zhuang Wang,Da Wang, Xinyu Yao, Yuan Meng,Yang Li,Li Yang

Journal of Molecular Structure（2022）

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摘要

•Seven new polymyxin E analogs are synthesized by hydrophobic modifaction Thr residue.•Hydrophobic modification of polymyxin E could enlarge the antibacterial range.•Polymyxin E analogs kill bacteria by disrupting cell membrane system.•Log p (1–3) of polymyxin E analogs may confer them a wider antibacterial spectrum.•Hydrophobic modification polymyxin E reduces neurotoxicity and nephrotoxicity.

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关键词

Polymyxin E,Hydrophobic modification,Bacterial cell membrane,Toxicity,Gram-positive bacteria

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