| 摘要 |
The present invention relates to mono- or bicyclic compounds of the general formula <CHEM> wherein X<1> is -S- or -SO-; R<1> is hydrogen, halogen or lower alkyl, optionally substituted by halogen ; R<2> is hydrogen, hydroxy, amino, lower alkylamino, di-lower alkylamino, optionally substituted lower alkoxy or a group -OP; OP is an easily hydrolyzable group; R<3> is hydrogen, hydroxy, lower alkyl, halogen or a group -OP; R<4> is halogen, hydroxy or a group -OP; R<5> is hydrogen, cyano, optionally substituted esterified carboxy or optionally substituted amidated (thio)carboxy, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted heterocyclyl; R<6> is -NR<7>-A, -N=B or optionally substituted heterocyclyl, in which R<7> is hydrogen or lower alkyl, A is optionally substituted iminoyl, optionally substituted (thio)acyl, optionally substituted esterified carboxy, optionally substituted amidated (thio)carboxy or optionally substituted heterocyclyl and B is optionally substituted alkylidene; R<0> is cyano, optionally substituted esterified carboxy or optionally substituted heterocyclyl, or wherein R<0> and R<6> taken together represent a group -CO-O-Q-X<2>-N(R<7>)-, wherein R<7> is as above, and X<2> is (thio)carbonyl or heterocyclyl; Q is -CH(R<8>)- or -CH(R<8>)-W-; R<8> is hydrogen or optionally substituted lower alkyl, and W is optionally substituted mono-, di-, tri-, tetra- or pentamethylene, provided that when W is monomethylene X<2> is other than (thio)carbonyl, and pharmaceutically acceptable salts of the mono- or bicyclic compounds of formula I carrying an acidic and/or basic substituent. The invention includes monocyclic compounds of the general formula <CHEM> wherein the substituents are as previously described, R<6> and R<0> being taken separatly, and bicyclic compounds of the general formula <CHEM> wherein the substituents are as previously described. These compounds of formula I as well as their pharmaceutically acceptable salts inhibit DNA gyrase activity in bacteria and possess antibiotic, especially antibacterial activity against microorganisms and can be used in the control or prevention of infectious diseases. |
