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- W2718087286 abstract "A new series of semisynthetic flavone-based small molecules mimicking antimicrobial peptides has been designed from natural icaritin to combat drug-resistant Gram-positive bacterial infections. Compound 6 containing two arginine residues exhibited excellent antibacterial activity against Gram-positive bacteria, including MRSA, and very low toxicity to mammalian cells, resulting in a high selectivity of more than 511, comparable to that of several membrane-active antibiotics in clinical trials. Our data show for the first time that icaritin derivatives effectively kill bacteria. Meanwhile, this is the first study deploying a biomimicking strategy to design potent flavone-based membrane targeting antimicrobials. 6 showed rapid bactericidal activity by disrupting the bacterial membrane and can circumvent the development of bacterial resistance. Importantly, 6 was highly efficacious in a mouse model of corneal infection caused by MRSA and Staphylococcus aureus." @default.
- W2718087286 created "2017-06-30" @default.
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- W2718087286 date "2017-07-07" @default.
- W2718087286 modified "2023-10-15" @default.
- W2718087286 title "Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant<i>Staphylococcus aureus</i>(MRSA)" @default.
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- W2718087286 doi "https://doi.org/10.1021/acs.jmedchem.7b00380" @default.
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