期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 14, 期 24, 页码 8506-8518出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.08.037
关键词
efflux pump inhibitor; MexAB-OprM efflux pump; Pseudomonas aeruginosa; drug resistance
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. (c) 2006 Elsevier Ltd. All rights reserved.
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