Conformationally-restricted analogues of efflux pump inhibitors that potentiate the activity of levofloxacin in Pseudomonas aeruginosa
Conformationally-restricted analogues of efflux pump inhibitors that potentiate the activity of levofloxacin in Pseudomonas aeruginosa
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DOI：
10.1016/s0960-894x(03)00556-0
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发表时间：
2003-08-18
影响因子：
2.7
通讯作者：
Ishida, Y
中科院分区：
文献类型：
--
作者：
Renau, TE;Léger, R;Ishida, Y
外排泵抑制剂D-ornithine-D-homophenylalanine-3-aminoquinoline(MC-02595-2)的鸟氨酸残基的构象限制提供了体内毒性较小的生物等构型脯氨酸衍生物，并且通过抑制铜绿假单胞菌的外排泵而与铅一样有效地增强了氟喹诺酮类左氧氟沙星的活性。(C)2003爱思唯尔有限公司。保留所有权利。
Conformational restriction of the ornithine residue of the efflux pump inhibitor D-ornithine-D-homophenylalanine-3-aminoquinoline (MC-02 595 2) furnished bioisosteric proline derivatives that were less toxic in vivo and as active as the lead in potentiating the activity of the fluoroquinolone levofloxacin via the inhibition of efflux pumps in Pseudomonas aeruginosa. (C) 2003 Elsevier Ltd. All rights reserved.