The Development And Biological Research Of Cephalosporin New Compounds

Cephalosporin antibiotics were not only the most usefully but also the most effectively clinical antimicrobial agents. From the first generation to the fourth, its marketing amount was always on the first place. But the bacterial resistance became the most important problem to slove. And research is needed to develop new kinds of cephalosporin antibiotic compounds.In this thesis, the 1-substituted and 2-substituted on the cephalosporin nucleus was designed and validated. Such transformation has not been studied. So there were only some reports. If the sulfur on 1-substituted was changed, theβ-lactamase became inhibition. And if it had 2-substituted,then this compound had moderate antimicrobial activity. We used GCLE as the beginning material, through six steps , the 2-substituted cephalosporin intermediate had been synthesized. And it would become a new platform for synthesizing a series of new 2-substituted cephalosporin intermediate. We could get some sulfur oxides andβ-lactamase affinity capacity data by the computer simulation. And the data displayed that the compounds of sulfur oxides had stronger binding force. We researched six new compounds, and the results were the same as the computer simulation.The structures of the key intermediates and the target product were confirmed by the analysis of 1H-NMR data.