- Studies on quinolone antibacterials. V. Synthesis and antibacterial activity of chiral 5-amino-7-(4-substituted-3-amino-1-pyrrolidinyl)-6- fluoro-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acids and derivatives
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We previously demonstrated that 5-amino-7-(3-amino1l-pyrrolidinyl)-1- cyclopropyl-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid (7) has strong in vitro antibacterial activity even against quinolone-resistant bacteria. We examined optimization of t
- Yoshida, Toshihiko,Yamamoto, Yoichi,Orita, Hitomi,Kakiuchi, Masato,Takahashi, Yoshie,Itakura, Masakazu,Kado, Noriyuki,Yasuda, Shingo,Kato, Hideo,Itoh, Yasuo
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- Process for producing quinolonecarboxlic acids and intermediates thereof
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This invention relates to methods for the efficient production of quinolonecarboxylic acid based synthetic antibacterial agents which are expected for applications such as excellent medicaments and agricultural chemicals and to intermediate compounds to be used therein. According to the present invention, an amine substituent as the 7-position substituent of the quinolonecarboxylic acid derivative can be efficiently introduced.
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- 5-amino-8-methyl-7-pyrrolidinylquinoline-3-carboxylic acid derivative
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A 5-amino-8-methyl-7-pyrrolidinylquinoline-3-carboxylic acid derivative represented by the general formula: STR1 wherein R1 is a hydrogen atom or a lower alkyl group; R2 is a hydrogen atom, a lower alkyl group, a lower alkanoyl group, a halogenated lower alkanoyl group or a residue of carboxylic acid ester; R3 is a hydrogen atom or a lower alkyl group; R4, R5 or R6 are each independently a hydrogen atom or a lower alkyl group; or two of R4, R5 and R6 may be taken together to form a --(CH2)n -group wherein n is 1 or 2, a stereoisomer thereof, or a pharmacologically acceptable salt thereof, the process for preparing these compounds, a pharmaceutical composition comprising an effective amount of these compounds and methods for the treatment of infectious diseases through the administration to patients of an effective amount of these compounds, and intermediates of these compounds are disclosed. These compounds are effective as antibacterial agents.
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