Journal of Medicinal Chemistry p. 1645 - 1656 (1990)
Update date:2022-08-05
Topics:
Miyamoto, Teruyuki
Matsumoto, Jun-ichi
Chiba, Katsumi
Egawa, Hiroshi
Shibamori, Koh-ichiro
et al.
A series of 5,7-disubstituted 1-cyclopropyl-6,8-difluoro-4(1H)-oxoquinoline-3-carboxylic acids (10-36) were prepared; the C-5 substituent in these compounds comprised halo, hydroxy, mercapto, and amino groups and the C-7 functional group included variously substituted piperazines.In vitro antibacterial screening results indicated that the amino group was optimal among the C-5 substituents.A combination of the C-5 amino group and the C-7 3,5-dimethylpiperazinyl appendage in this series conferred the best overall antibacterial property with lack of adverse drug interactions.Compound 36k
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