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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.

✍ Scribed by S. J. YOON; Y. H. CHUNG; C. W. LEE; Y. S. OH; D. R. CHOI; N. D. KIM; J. K. LIM; Y. H. JIN; D. K. LEE; W. Y. LEE

Publisher: John Wiley and Sons
Year: 2010
Weight: 35 KB
Volume: 28
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.199745165

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✦ Synopsis

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 synthesized and evaluated for their antibacterial activity. Derivative (VIIIa) displays a moderate in vitro antibacterial activity, but it shows very excellent pharmacokinetic profiles, so that (VIIIa) shows dramatic increased in vivo efficacy. -(YOON, S.

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