Bioorganic and Medicinal Chemistry Letters p. 1953 - 1958 (1998)
Update date:2022-08-03
Topics: Steric and Electronic Effects Substituent Effects Toxicity and Selectivity
Li, Qun
Wang, Weibo
Berst, Kristine B.
Claiborne, Akiyo
Hasvold, Lisa
Raye, Kathleen
Tufano, Michael
Nilius, Angela
Shen, Linus L.
Flamm, Robert
Alder, Jeff
Marsh, Kennan
Crowell, DeAnne
Chu, Daniel T.W.
Planner, Jacob J.
The 8-position side chain of 2-pyridones is believed to be involved in the binding with bacterial DNA gyrase to form the ternary complex, making them very important for the activity of 2-pyridones. A series of 2-pyridones having fluoro-substituted amines at the 8-position has been synthesized and their antibacterial activities and parmacokinetic properties are reported.
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