Title of article
MexAB-OprM-Specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 1: Discovery and early strategies for lead optimization
Author/Authors
Kiyoshi Nakayama، نويسنده , , Yohei Ishida، نويسنده , , Masami Ohtsuka، نويسنده , , Haruko Kawato، نويسنده , , Ken-ichi Yoshida and Shoichi Kobayashi، نويسنده , , Yoshihiro Yokomizo، نويسنده , , Shigeru Hosono، نويسنده , , Toshiharu Ohta، نويسنده , , Kazuki Hoshino، نويسنده , , Hiroko Ishida، نويسنده , , Kumi Yoshida، نويسنده , , Thomas E. Renau، نويسنده , , Roger Léger، نويسنده , , Jason Z. Zhang، نويسنده , , Ving J. Lee، نويسنده , , William J. Watkins، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
4
From page
4201
To page
4204
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793750
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