MexAB-OprM-specific efflux pump inhibitors in Pseudomonas aeruginosa.: Part 1:: Discovery and early strategies for lead optimization
MexAB-OprM-specific efflux pump inhibitors in Pseudomonas aeruginosa.: Part 1:: Discovery and early strategies for lead optimization
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DOI：
10.1016/j.bmcl.2003.07.024
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发表时间：
2003-12-01
影响因子：
2.7
通讯作者：
Watkins, WJ
中科院分区：
文献类型：
--
作者：
Nakayama, K;Ishida, Y;Watkins, WJ
鉴定了一系列特异性抑制铜绿假单胞菌MexAB-OprM泵系统外排的化合物。概述了合成和体外结构-活性关系（SAR）。早期的铅缺乏活动的动物模型，并努力提高溶解度和减少血清蛋白结合的极性基团的介绍进行了讨论。(C)2003爱思唯尔有限公司。保留所有权利。
The identification of a series of compounds that specifically inhibit efflux by the MexAB-OprM pump system in Pseudomonas aeruginosa is described. Synthesis and in vitro structure-activity relationships (SARs) are outlined. Early leads lacked activity in animal models, and efforts to improve solubility and reduce serum protein binding by the introduction of polar groups are discussed. (C) 2003 Elsevier Ltd. All rights reserved.