Synthesis and Structure-Activity Relationship Studies of N-Terminal Analogues of the Antimicrobial Peptide Tridecaptin A1
Synthesis and Structure-Activity Relationship Studies of N-Terminal Analogues of the Antimicrobial Peptide Tridecaptin A1
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DOI：
10.1021/jm401779d
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发表时间：
2014-02-13
影响因子：
7.3
通讯作者：
Vederas, John C.
中科院分区：
文献类型：
--
作者：
Cochrane, Stephen A.;Lohans, Christopher T.;Vederas, John C.
化学合成用于增加抗微生物脂肽tridecaptin A（1）的效力。脂质尾部修饰被证明是合成结构上更简单的类似物的理想平台，这些类似物不易通过分离获得。tridecaptin A（1）脂质尾部的立体化学元素对于抗微生物活性不是必需的，并且可以被疏水脂肪族或芳香族基团取代。一些更简单的类似物显示出对革兰氏阴性菌的有效抗菌活性，包括空肠弯曲杆菌、大肠杆菌O157：H7和多重耐药肺炎克雷伯菌。
Chemical synthesis was used to increase the potency of the antimicrobial lipopeptide tridecaptin A(1). Lipid tail modification proved to be an ideal platform for synthesizing structurally simpler analogues that are not readily accessible by isolation. The stereochemical elements of the tridecaptin A(1) lipid tail are not essential for antimicrobial activity and could be replaced with hydrophobic aliphatic or aromatic groups. Some simpler analogues displayed potent antimicrobial activity against Gram-negative bacteria, including Campylobacter jejuni, Escherichia coli O157:H7, and multidrug resistant Klebsiella pneumoniae.