| 摘要 |
<p>The present invention relates to novel quinoline derivatives of formula (I): <CHEM> wherein, R1 is a straight chain or cyclic lower alkyl group having 1 to 3 carbon atoms, a straight chain or cyclic lower alkyl group having 1 to 3 carbon atoms which is substituted with a halogen atom, a phenyl group or a phenyl group substituted with one or two halogen atoms; R2 is a hydrogen atom, a lower alkyl or amino group; R3 is a halogen atom or a substituted or unsubstituted heterocyclic group represented by the following formula (A) which contains at least one nitrogen atom as a hetero atom in the ring; <CHEM> wherein, R6, R7, R8 and R9 are each hydrogen atoms or lower alkyl groups, or two of these groups may form a bond, m and n are 0 or 1, and Ca-Cb may not form a bond, or is single or double bond; X is nitrogen atom or C-R4 wherein R4 is hydrogen or halogen atom, or lower alkyl or lower alkoxy group; and Y and Z are each hydrogen atoms, or electron withdrawing groups, for example, ester, cyano, nitro, acyl or substituted acyl, substituted or unsubstituted amide, lower alkylsulfoxy or lower alkylsulfonyl group, and pharmaceutically acceptable acid addition salts thereof, and also to processes for preparing these compounds. The present invention also provides an antibacterial composition comprising a compound of formula (I) or its acid addition salt as an active ingredient and pharmaceutically acceptable excipients. The novel quinoline derivatives of the present invention have an excellent antibacterial activity against bacteria or bacteroides.</p> |
