基于多粘菌素 B 七肽的细菌外膜通透剂的构效关系。
Structure-activity relationships of bacterial outer-membrane permeabilizers based on polymyxin B heptapeptides.
机构信息
Department of Chemistry and Chemical Biology, Gunma University, 1-5-1 Tenjin-cho, Kiryu, Gunma 376-8515, Japan.
出版信息
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1771-5. doi: 10.1016/j.bmcl.2010.01.040. Epub 2010 Jan 20.
A series of cationic cyclic heptapeptides based on polymyxin B have been synthesized for use as permeabilizers of the outer membrane of Gram-negative bacteria. Only analogs with the Dab(2)-d-Phe(3)-Leu(4)-Xxx(5) sequence (Xxx = Dab or Orn) showed a synergistic bactericidal effect when combined with conventional antibiotics, indicating that the Dab(2) residue plays a critical role in permeation of the outer membrane of Gram-negative bacteria.
已经合成了一系列基于多粘菌素 B 的阳离子环状七肽，用作革兰氏阴性菌外膜的通透剂。只有具有 Dab(2)-d-Phe(3)-Leu(4)-Xxx(5)序列（Xxx = Dab 或 Orn）的类似物与常规抗生素联合使用时表现出协同杀菌作用，这表明 Dab(2)残基在外膜渗透中起着关键作用革兰氏阴性菌。
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