铜绿假单胞菌中MexAB-OprM特异性外排泵抑制剂。第5部分：C-2位的碳取代类似物。
MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 5: Carbon-substituted analogues at the C-2 position.
作者信息
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
机构信息
Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co., Ltd, 16-13, Kita-Kasai 1-Chome, Tokyo 134-8630, Japan.
出版信息
Bioorg Med Chem. 2006 Mar 15;14(6):1993-2004. doi: 10.1016/j.bmc.2005.10.043. Epub 2005 Nov 15.
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 beta-lactam aztreonam (AZT) in Pseudomonas aeruginosa. Palladium-catalyzed cross-coupling methods were applied for the incorporation of aliphatic and aromatic substituents.
合成了一系列在2位带有碳连接取代基的4-氧代-4H-吡啶并[1,2-a]嘧啶衍生物，并评估了它们增强氟喹诺酮左氧氟沙星（LVFX）和抗铜绿假单胞菌β-内酰胺氨曲南（AZT）在铜绿假单胞菌中活性的能力。采用钯催化交叉偶联方法引入脂肪族和芳香族取代基。
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