申请人:Korea Institute of Science and Technology
公开号:US05675003A1
公开(公告)日:1997-10-07
A 3-ammoniopropenyl cephalosporin of the following formula (I): ##STR1## wherein P is hydroxylated alicyclic or aliphatic amines such as meso-3,4-dihydroxy-1-methylpyrrolidine, (3S,4S)-3,4-dihydroxy-1-methylpyrrolidine, (3R,4R)-3,4-dihydroxy-1-methylpyrrolidine, rac-3,4-trans-dihydroxy-1-methylpyrrlidine, (2S,4R)-4-hydroxy-1-methyl-2-pyrrolidinemethanol, N-methyl-bis(2-hydroxyethyl)amine, 3,4-cis-dihydroxy-1-methylpiperidine, 3,4-trans-dihydroxypiperidine, 4-hydroxy-1-methylpiperidine, 2-hydroxymethyl-1-methylpiperidine, or tropine, or a pharmaceutically acceptable salt thereof, exhibits good anti-bacterial activities against a wide variety of Gram-positive and Gram-negative bacteria; and a process for the preparation thereof.
一种具有下述通式(I)的3-氨丙烯基头孢菌素:##STR1##其中P为羟基化的脂环族或脂族胺,如meso-3,4-二羟基-1-甲基吡咯烷、(3S,4S)-3,4-二羟基-1-甲基吡咯烷、(3R,4R)-3,4-二羟基-1-甲基吡咯烷、消旋-3,4-反式-二羟基-1-甲基吡咯啉、(2S,4R)-4-羟基-1-甲基-2-吡咯烷甲醇、N-甲基-双(2-羟乙基)胺、3,4-顺式-二羟基-1-甲基哌啶、3,4-反式-二羟基哌啶、4-羟基-1-甲基哌啶、2-羟甲基-1-甲基哌啶或托品,或其药学上可接受的盐,对多种革兰氏阳性和革兰氏阴性细菌表现出良好的抗菌活性;以及其制备方法。