90679-45-1Relevant academic research and scientific papers
Pyridonecarboxylic acids as antibacterial agents. 9. Synthesis and antibacterial activity of 1-substituted 6-fluoro-1,4-dihydro-4-oxo-7-(4-pyridyl)-1,8-naphthyridine-3-carb oxylic acids
Nishimura,Matsumoto
, p. 1622 - 1626 (1987)
The title compounds (7a-e) with ethyl, 2-fluoroethyl, 2-hydroxyethyl, vinyl, or cyclopropyl groups, respectively, at C-1 were prepared by the method involving the Balz-Schiemann reaction of 2-(4-pyridyl)pyridine- and 7-(4-pyridyl)-1,8-naphthyridinediazonium tetrafluoroborates (15 and 27). The 1-ethyl, 1-(2-fluoroethyl), and 1-vinyl derivatives showed in vitro activities as potent as the corresponding 7-(1-piperazinyl) analogues against Staphylococcus aureus 209P JC-1 and Escherichia coli NIHJ JC-2 but were less active against Pseudomonas aeruginosa 12. Among the 7-(4-pyridyl) derivatives having the different C-1 substituent, 1-cyclopropyl derivative 7e was found to be the most active. In vivo efficacy of 7e was superior to that of enoxacin against experimental infections due to S. aureus 50774. Some aspects of structure-activity relationships associated with the C-1, C-6, and C-7 substituents were discussed.
7-(4-Pyridyl)-1,8-naphthyridine derivatives and their antibacterial compositions
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, (2008/06/13)
A 7-(4-pyridyl)-1,8-naphthyridine compound of the formula STR1 wherein R1 is a hydrogen atom, an ethyl or vinyl group, and R2 is a hydrogen atom or a lower alkyl group having 1 to 6 carbon atoms, and a salt thereof. The compounds represented by the formula are useful in antibacterial compositions or intermediates thereof.
