475062-07-8Relevant academic research and scientific papers
MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 7: Highly soluble and in vivo active quaternary ammonium analogue D13-9001, a potential preclinical candidate
Yoshida, Ken-ichi,Nakayama, Kiyoshi,Ohtsuka, Masami,Kuru, Noriko,Yokomizo, Yoshihiro,Sakamoto, Atsunobu,Takemura, Makoto,Hoshino, Kazuki,Kanda, Hiroko,Nitanai, Hironobu,Namba, Kenji,Yoshida, Kumi,Imamura, Yuichiro,Zhang, Jason Z.,Lee, Ving J.,Watkins, William J.
, p. 7087 - 7097 (2008/04/12)
A series of 4-oxo-4H-pyrido[1,2-a]pyrimidine derivatives, substituted at the 2-position with piperidines bearing quaternary ammonium salt side chains, were synthesized and evaluated for their ability to potentiate the activity of the fluoroquinolone levofloxacin (LVFX) and the β-lactam aztreonam (AZT) in Pseudomonas aeruginosa. Attachment of the charged entity using an N-ethylcarbamoyloxy linker led to the discovery of the highly soluble compound 22 (D13-9001), which maintained good potency in vitro and displayed excellent activity in vivo in a rat pneumonia model of P. aeruginosa.
