Addressing the stability of C-capped dipeptide efflux pump inhibitors that potentiate the activity of levofloxacin in Pseudomonas aeruginosa

被引：50
作者：
Renau, TE
Léger, R
Flamme, EM
She, MW
Gannon, CL
Mathias, KM
Lomovskaya, O
Chamberland, S
Lee, VJ
Ohta, T
Nakayama, K
Ishida, Y
机构：
[1] Microcide Pharmaceut 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 | 2001年 / 11卷 / 05期
关键词：
D O I：
10.1016/S0960-894X(01)00033-6
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Synthetic optimization of a biologically labile class of dipeptides that function as efflux pump inhibitors to potentiate the antibacterial agent levofloxacin in Pseudomonas aeruginosa has led to the discovery of a related series of compounds that are completely stable in a variety of biological matrices. Other than the stability profile, the in vitro profile of the new series is essentially identical to that observed with the original one. A prototypical compound from the new series demonstrates potentiation in an in vivo model of infection. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：663 / 667
页数：5
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