| 摘要 |
RAN 4410/223 Carbapenem compounds of the general formula I wherein R is hydrogen or a carboxylic acid protecting group; R1 is selected from the group consisting of hydrogen, lower alkyl, lower alkoxy and hydroxyalkyl; R2 and R3 are each independently hydrogen, lower alkyl, lower alkoxy or lower alkylthio; and Y is (i) an ester group; (ii) a thioester group; (iii) a piperazinyl or pyrrolidinyl derived carbamate group; (iv) a piperazinyl derived amine group; (v) a piperazinyl derived quaternary ammonium group: or (vi) a group comprising a covalent bond; the ester group and the thioester group being bonded to a substituted quinolonyl or naphthyridonyl group; the piperazinyl or pyrrolidinyl derived carbamate group, the piperazinyl derived amine group and the piperazinyl derived quaternary ammonium group containing a piperazinyl nucleus or a eyrrolidinyl nucleus having a nitrogen atom bonded directly to a substituted quinolonyl or naphthyridonyl group, the piperazinyl and the pyrrolidinyl nuclei being unsubstituted or substituted with one or more lower alkyl groups; and the covalent bond of the corresponding group being connected to a substituted isothiazolo or isoxazolo quinolonyl or naphthyridonyl group via a nitrogen atom in an isothiazolo or isoxazolo nucleus: as well as the corresponding readily hydrolyzable esters, pharmaceutically acceptable salts and hydrates of any of the foregoing compounds. The products have antibacterial activity.
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