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具有抗金黄色葡萄球菌活性的脂肽 Battacin 的线性类似物。

Linear Analogues of the Lipopeptide Battacin With Potent In Vitro Activity Against S. aureus.

机构信息

School of Chemical Sciences, The University of Auckland, Auckland, New Zealand.

School of Chemical Sciences, The University of Auckland, Auckland, New Zealand.

出版信息

Adv Protein Chem Struct Biol. 2018;112:385-394. doi: 10.1016/bs.apcsb.2018.03.004. Epub 2018 Apr 6.

Abstract

Eight linear analogues of the lipopeptide battacin were evaluated for their antibacterial activity against the Gram-positive Staphylococcus aureus. Of this library, the enantiomeric lipopeptide analogue 9.4 exhibited nanomolar inhibitory activity (MIC=200nmol) against S. aureus. Furthermore, this lipopeptide was resilient toward degradation conditions when exposed to rat serum proteases for up to 8h.

摘要

评估了 8 个线性类似物的脂肽 battacin 的抗菌活性,以对抗革兰氏阳性金黄色葡萄球菌。在这个文库中,对映体脂肽类似物 9.4 对金黄色葡萄球菌表现出纳摩尔抑制活性(MIC=200nmol)。此外,这种脂肽在暴露于大鼠血清蛋白酶长达 8 小时的情况下,对降解条件具有弹性。

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