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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
Author(s) -
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
Publication year - 1997
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570340348
Subject(s) - chemistry , antibacterial activity , pharmacokinetics , in vivo , in vitro , carboxylic acid , stereochemistry , biological activity , antibacterial agent , combinatorial chemistry , bacteria , organic chemistry , pharmacology , antibiotics , biochemistry , medicine , genetics , microbiology and biotechnology , biology
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.