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

页码：663 / 667

页数：5