| Literature DB >> 16979895 |
Ken-ichi Yoshida1, Kiyoshi Nakayama, Yoshihiro Yokomizo, Masami Ohtsuka, Makoto Takemura, Kazuki Hoshino, Hiroko Kanda, Kenji Namba, Hironobu Nitanai, Jason Z Zhang, Ving J Lee, William J Watkins.
Abstract
A series of 4-oxo-4H-pyrido[1,2-a]pyrimidine derivatives, derivatized at the 2-position with aromatic substituents, were synthesized by the Suzuki cross-coupling method and evaluated for their ability to potentiate the activity of the fluoroquinolone levofloxacin (LVFX) and the anti-pseudomonas beta-lactam aztreonam (AZT) in Pseudomonas aeruginosa. By incorporating hydrophilic substituents onto the aryl nucleus, we found a morpholine analogue that possessed improved solubility, retained activity in vitro, and displayed potentiation activity in vivo in a rat model of P. aeruginosa pneumonia.Entities:
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Year: 2006 PMID： 16979895 DOI： 10.1016/j.bmc.2006.08.037
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641