Quinoline carboxylic acid derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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540492, 540544, 540575, 540597, A61K 3155, C07D24308

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active

053859006

ABSTRACT:
A quinolone carboxylic acid derivative having the following formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group, an aralkyl group, an ester residual group which can be hydrolyzed in living bodies, R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two lower alkyl groups, X is a hydrogen atom or a halogen atom, Y is CH.sub.2, O, S, SO, SO.sub.2, or N--R.sup.3, wherein R.sup.3 is a hydrogen atom or a lower alkyl group, and Z is an oxygen atom or two hydrogen atoms; or a salt thereof; and an antimicrobial agent comprising the same. The compound exhibits a superior antimicrobial activity, especially against gram positive microorganisms, and is thus useful for the treatments and prevention of various infectious diseases in clinics.

REFERENCES:
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patent: 5140033 (1992-08-01), Schriewer et al.
Ito et al., Chemical Abstract, 110(5), 39031a, 1988.
Ito et al. Chemical Abstract, 109(15),129070W, 1988.
Journal of Medicinal Chemistry, vol. 33, 1990, pp.142-146, C. B. Ziegler, Jr. et al., "Synthesis and Structure-Activity Relationships of New 7[3-(Fluoromethyl)Piperazinyl]-and -(Fluorohomopiperazinyl) Quinoline Antibacterials".
Journal of Medicinal Chemistry, vol. 28, 1985, pp. 1558-1564, D. T. W. Chu, et al., "Synthesis and Structure-Activity Relationships of Novel Arylfluoroquinolone Antibacterial Agents".

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