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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

✍ Scribed by Sung June Yoon; Yong Ho Chung; Chi Woo Lee; Yoon Seok Oh; Dong Rack Choi; Nam Doo Kim; Jae Kyung Lim; Yoon Ho Jin; Dug Keun Lee; Won Yong Lee

Publisher: Journal of Heterocyclic Chemistry
Year: 1997
Tongue: English
Weight: 490 KB
Volume: 34
Category: Article
ISSN: 0022-152X
DOI: 10.1002/jhet.5570340348

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✦ Synopsis

Abstract

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.

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ChemInform Abstract: 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.

✍ S. J. YOON; Y. H. CHUNG; C. W. LEE; Y. S. OH; D. R. CHOI; N. D. KIM; J. K. LIM; 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 35 KB 👁 2 views

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. -A variety of new quinolones bearing fluorinated pyridyl groups at N1 ( cf. (VIII), (IX); 18 examples) are syn