475060-22-1Relevant articles and documents
MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 4: Addressing the problem of poor stability due to photoisomerization of an acrylic acid moiety
Nakayama, Kiyoshi,Kuru, Noriko,Ohtsuka, Masami,Yokomizo, Yoshihiro,Sakamoto, Atsunobu,Kawato, Haruko,Yoshida, Ken-Ichi,Ohta, Toshiharu,Hoshino, Kazuki,Akimoto, Katsuya,Itoh, Junko,Ishida, Hiroko,Cho, Aesop,Palme, Monica H.,Zhang, Jason Z.,Lee, Ving J.,Watkins, William J.
, p. 2493 - 2497 (2007/10/03)
Exchange of the ethylene tether in a series of pyridopyrimidine-based MexAB-OprM specific efflux pump inhibitors to an amide bond stabilized the olefin of the acrylic acid moiety, preventing facile photoisomerization to the Z-isomer. Furthermore, the activity was drastically improved in the amide tether variants, providing extremely potent acrylic acid and vinyl tetrazole analogues.