Synthesis and Structure-Activity Relationship Studies of N-Terminal Analogues of the Antimicrobial Peptide Tridecaptin A1

被引：58

作者：

Cochrane, Stephen A. ^{[1
]}

Lohans, Christopher T. ^{[1
]}

Brandelli, Jeremy R. ^{[2
]}

Mulvey, George ^{[2
]}

Armstrong, Glen D. ^{[2
]}

Vederas, John C. ^{[1
]}

机构：

[1] Univ Alberta, Dept Chem, Edmonton, AB T6G 2G2, Canada

[2] Univ Calgary, Dept Microbiol Immunol & Infect Dis, Calgary, AB T2N 4Z6, Canada

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 57卷 / 03期

基金：

加拿大自然科学与工程研究理事会;

关键词：

GENUS BACILLUS; ANTIBIOTICS;

D O I：

10.1021/jm401779d

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：1127 / 1131

页数：5