Synthesis and structure-activity relationships of 2-pyridones: a novel series of potent DNA gyrase inhibitors as antibacterial agents

…, KB Berst, P Donner, W Wang, L Hasvold…

文献索引：Li, Qun; Chu, Daniel T. W.; Claiborne, Akiyo; Cooper, Curt S.; Lee, Cheuk M.; Raye, Kathleen; Berst, Kristine B.; Donner, Pamela; Wang, Weibo; Hasvold, Lisa; Fung, Anthony; Ma, Zhenkun; Tufano, Michael; Flamm, Robert; Shen, Linus L.; Baranowski, John; Nilius, Angela; Alder, Jeff; Meulbroek, Jonathan; Marsh, Kennan; Crowell, DeAnne; Hui, Yuhua; Seif, Louis; Melcher, Laura M.; Henry, Rodger; Spanton, Steven; Faghih, Ramin; Klein, Larry L.; Tanaka, S. Ken; Plattner, Jacob J. Journal of Medicinal Chemistry, 1996 , vol. 39, # 16 p. 3070 - 3088

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被引用次数: 81

摘要

Two novel series of 2-pyridones were synthesized by transposition of the nitrogen of 4- quinolones to the bridgehead position. This subtle interchange of the nitrogen atom with a carbon atom yielded two novel heterocyclic nuclei, pyrido [1, 2-a] pyrimidine and quinolizine, which had not previously been evaluated as antibacterial agents and were found to be potent inhibitors of DNA gyrase. Quinolizines with a methyl group at the 9-position such as ...