Design,Synthesis And Antibacterial Activity Evaluation Of Ferruginol And Its Analogs

The abuse of antibiotics accelerates the process of bacterial drug resistance.At present,the study of antimicrobial drugs is relatively lagged,therefore,the development of new antimicrobial agents has become an urgent need.The antimicrobial activity of(+)-Ferruginol has been reported.(±)-Ferruginol and a series of its novel analogs had been synthesized based on the key cyclization reaction and their antibacterial activities were evaluated against Staphylococcus aureus,including Newman strains and multidrug-resistant strains(NRS-1,NRS-70,NRS-100,NRS-108 and NRS-271).The results showed that compounds 18,20,23and 37 displayed good inhibitory activities to those staphylococcus aureus strains with MIC values of 1.56-3.13?g/mL.Compounds 48,36,42,50 and 52 displayed excellent inhibitory activity to these staphylococcus aureus strains with MIC values of 0.78-3.13?g/mL.Among them compound 42 showed the best antimicrobial activity,which was more potent than(+)-Ferruginol and Kanamycin,and equivalent to Vancomycin and Totarol.The cytotoxic activities against human fibroblast(HAF)cells of selected compounds 18,36,37,42,48,50 and 52 were measured in vitro and their morphologies were also observed.The results showed that these compounds had no obvious toxicity to the normal HAF cells at the MIC concentration.Work of this thesis provides high-quality lead compounds for the study of new antibacterial angents.