Conformationally-restricted analogues of efflux pump inhibitors that potentiate the activity of levofloxacin in Pseudomonas aeruginosa

被引：82
作者：
Renau, TE
Léger, R
Filonova, L
Flamme, EM
Wang, M
Yen, R
Madsen, D
Griffith, D
Chamberland, S
Dudley, MN
Lee, VJ
Lomovskaya, O
Watkins, WJ
Ohta, T
Nakayama, K
Ishida, Y
机构：
[1] Essential Therapeut Inc, Mountain View, CA 94043 USA
[2] Daiichi Pharmaceut Co Ltd, New Prod Res Labs 1, Tokyo 1348630, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 16期
关键词：
D O I：
10.1016/S0960-894X(03)00556-0
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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.
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页码：2755 / 2758
页数：4
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