113191-99-4Relevant academic research and scientific papers
MexAB-OprM-specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 1: Discovery and early strategies for lead optimization
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.,Leger, Roger,Zhang, Jason Z.,Lee, Ving J.,Watkins, William J.
, p. 4201 - 4204 (2007/10/03)
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
DRUG DISCHARGE PUMP INHIBITORS
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, (2008/06/13)
A medicament for preventive and/or therapeutic treatment of a microbial infection having an activity of eliminating resistance of a microorganism with acquired resistance to an antimicrobial agent, which comprises as an active ingredient a compound represented by the following general formula (I), a physiologically acceptable salt thereof, or a hydrate thereof: wherein R1 and R2 independently represent hydrogen atom, a halogen atom, carboxyl group and the like; J1 represents a 5- or 6-membered heteroaromatic ring; W1 represents -CH=CH-, -C≡C-, -CH2CH2- and the like; A1 represents phenylene group, pyridinediyl group, furandiyl group and the like; G1 represents oxygen atom, carbonyl group, ethynyl group and the like; p represents an integer of from 0 to 3; G2 represents phenylene group, furandiyl group, tetrahydrofurandiyl group and the like; G3 represents -CH2- or single bond; m and n represent an integer of 0 or 1; and Q1 represents an acidic group.
