MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 5: Carbon-substituted analogues at the C-2 position

K Yoshida, K Nakayama, N Kuru, S Kobayashi…

Index: Yoshida, Ken-Ichi; Nakayama, Kiyoshi; Kuru, Noriko; Kobayashi, Shozo; Ohtsuka, Masami; Takemura, Makoto; Hoshino, Kazuki; Kanda, Hiroko; Zhang, Jason Z.; Lee, Ving J.; Watkins, William J. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 6 p. 1993 - 2004

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Citation Number: 46

Abstract

A series of 4-oxo-4H-pyrido [1, 2-a] pyrimidine derivatives, derivatized at the 2-position with carbon-linked substituents, were synthesized and evaluated for their ability to potentiate the activity of the fluoroquinolone levofloxacin (LVFX) and the anti-pseudomonas β-lactam aztreonam (AZT) in Pseudomonas aeruginosa. Palladium-catalyzed cross-coupling methods were applied for the incorporation of aliphatic and aromatic substituents.