Antimicrobial Activity of Peptidomimetics against Multidrug-Resistant Escherichia coli: A Comparative Study of Different Backbones

被引:66
|
作者
Jahnsen, Rasmus D. [1 ]
Frimodt-Moller, Niels [2 ]
Franzyk, Henrik [1 ]
机构
[1] Univ Copenhagen, Fac Hlth & Med Sci, Dept Drug Design & Pharmacol, DK-2100 Copenhagen, Denmark
[2] Hvidovre Univ Hosp, Dept Microbiol, DK-2650 Hvidovre, Denmark
关键词
HOST-DEFENSE PEPTIDES; SOLID-PHASE SYNTHESIS; PEPTOID OLIGOMERS; DESIGN; ANTIBACTERIAL; BACTERIA; SEQUENCE; MECHANISM;
D O I
10.1021/jm300820a
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Novel remedies in the battle against multidrug-resistant bacterial strains are urgently needed, and one obvious approach involves antimicrobial peptides and mimics hereof. The impact of alpha- and beta-peptoid as well as beta(3)-amino acid modifications on the activity profile against beta-lactamase-producing Escherichia coli was assessed by testing an array comprising different types of cationic peptidomimetics obtained by a general monomer-based solid-phase synthesis protocol. Most of the peptidomimetics possessed high to moderate activity toward multidrug-resistant E. coli as opposed to the corresponding inactive peptides. Nevertheless, differences in hemolytic activities indicate that a careful choice of backbone design constitutes a significant parameter in the search for effective cationic antimicrobial peptidomimetics targeting specific bacteria.
引用
收藏
页码:7253 / 7261
页数:9
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