… as antibacterial agents. 4. Synthesis and structure-activity relationships of 5-substituted 6-fluoro-7-(cycloalkylamino)-1, 4-dihydro-4-oxo-1, 8-naphthyridine-3- …

D Bouzard, P Di Cesare, M Essiz…

文献索引：Bouzard, D.; Cesare, P. Di; Essiz, M.; Jacquet, J. P.; Ledoussal, B.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 3 p. 518 - 525

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被引用次数: 78

摘要

A series of 5-substituted-6-fluoro-7-(cycloalkylamino)-l, 4-dihydro-4-oxo-l, &naphthyridine-3- carboxylic acids have been prepared and tested for their in vitro and in vivo antibacterial activities. The 5-methyl group gave better in vitro activity with the 1-cyclopropyl appendage, but poorer activity with the 1-tert-butyl moiety. With the 1-(2, 4-difluorophenyl) substitution, the influence of the 7-cycloalkylamino group was determinant: a (3S)-3-aminopyrrolidine ...