Chemical and Pharmaceutical Bulletin p. 2063 - 2070 (1994)
Update date:2022-08-02
Topics:
Todo
Nitta
Miyajima
Fukuoka
Yamashiro
Nishida
Saikawa
Narita
4-Oxo-1,8-naphthyridine- and 4-oxoquinoline-3-carboxylic acids (2a, b and 3a-l) possessing a 1-aminocyclopropyl group at the 7-position have been synthesized and evaluated for in vitro antibacterial activities. The three quinolones (3d, h, i) exhibited potent antibacterial activities against both gram-positive and gram-negative bacteria, which are comparable to those of ciprofloxacin (CPFX) and ofloxacin (OFLX). Among the three compounds, the best pharmacological and pharmacokinetic profile was obtained with 3i, an OFLX analogue, which was considerably less toxic than three reference quinolones (1, CPFX, and OFLX).
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Doi:10.1016/S0040-4020(01)90543-5
(1990)Doi:10.1021/ol101406k
(2010)Doi:10.1002/recl.19881070407
(1988)Doi:10.1039/c0cc00650e
(2010)Doi:10.1021/om100388w
(2010)Doi:10.1021/ol101176j
(2010)