Synthesis, pharmacokinetics, and biological activity of a series of new pyridonecarboxylic acid antibacterial agents bearing a 5-fluoro-2-pyridyl group or a 3-fluoro-4-pyridyl group at N-1

Synthesis, pharmacokinetics, and biological activity of a series of new pyridonecarboxylic acid antibacterial agents bearing a 5-fluoro-2-pyridyl group or a 3-fluoro-4-pyridyl group at N-1

The 1‐(5‐fluoro‐2‐pyridyl) or 1‐(3‐fluoro‐4‐pyridyl) group was introduced in the syntheses of new pyridonecarboxylic acid antibacterial agents. 1‐(5‐Fluoro‐2‐pyridyl)‐6‐fluoro‐1,4‐dihydro‐7‐(4‐methyl‐1‐piperazinyl)‐4‐oxoquinolone‐3‐carboxylic acid 7b (DW‐116) showed a moderate in vitro antibacterial...

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Veröffentlicht in:Journal of heterocyclic chemistry 1997-05, Vol.34 (3), p.1021-1027
Hauptverfasser: Yoon, Sung June, Chung, Yong Ho, Lee, Chi Woo, Oh, Yoon Seok, Choi, Dong Rack, Kim, Nam Doo, Lim, Jae Kyung, Jin, Yoon Ho, Lee, Dug Keun, Lee, Won Yong
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container_end_page 1027
container_issue 3
container_start_page 1021
container_title Journal of heterocyclic chemistry
container_volume 34
creator Yoon, Sung June
Chung, Yong Ho
Lee, Chi Woo
Oh, Yoon Seok
Choi, Dong Rack
Kim, Nam Doo
Lim, Jae Kyung
Jin, Yoon Ho
Lee, Dug Keun
Lee, Won Yong
description The 1‐(5‐fluoro‐2‐pyridyl) or 1‐(3‐fluoro‐4‐pyridyl) group was introduced in the syntheses of new pyridonecarboxylic acid antibacterial agents. 1‐(5‐Fluoro‐2‐pyridyl)‐6‐fluoro‐1,4‐dihydro‐7‐(4‐methyl‐1‐piperazinyl)‐4‐oxoquinolone‐3‐carboxylic acid 7b (DW‐116) showed a moderate in vitro antibacterial activity but it was found to have very excellent pharmacokinetic profiles so that 7b (DW‐116) showed dramatic increased in vivo efficacy.
doi_str_mv 10.1002/jhet.5570340348
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title Synthesis, pharmacokinetics, and biological activity of a series of new pyridonecarboxylic acid antibacterial agents bearing a 5-fluoro-2-pyridyl group or a 3-fluoro-4-pyridyl group at N-1
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