|
|||||
|
|
MexAB-OprM-specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 1: discovery and early strategies for lead optimization |
|
| Authors: | Nakayama Kiyoshi Ishida Yohei Ohtsuka Masami Kawato Haruko Yoshida Ken ichi Yokomizo Yoshihiro Hosono Shigeru Ohta Toshiharu Hoshino Kazuki Ishida Hiroko Yoshida Kumi Renau Thomas E Léger Roger Zhang Jason Z Lee Ving J Watkins William J |
| Institution: | Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co., Ltd., 1-16-13, Kitakasai, Edogawa, Tokyo, 134-8630, Japan. nakaygoi@daiichipharm.co.jp |
| Abstract: | 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. |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |