新型9-肟醚3-红霉素酰内酯的研究

【作者】 李汉兵； 张涛； 姜凤超；

【机构】 华中科技大学同济医学院药学院；

【摘要】 目的寻找具有良好药代动力学性质和抗耐药性的新一代红霉素衍生物。方法根据红霉素作用机理和构效关系,设计并合成了3个新的含氨基酸取代基的红霉素衍生物,并用常规二倍稀释法对制备的目标化合物进行了体外抗菌活性的检测。结果与结论体外抗菌试验表明设计并合成的三个化合物均显示了较好的抗菌活性,特别是对红霉素耐药的肺炎链球菌有良好的敏感性。更多还原

【Abstract】 Aim To discover new erythromycin A derivatives with good pharmacokinetic profiles and anti-tolerance. Methods According to antibacterial mechanism and structure-activity relationship(SAR) of erythromycin A, three new derivatives with amino acid tethered to C-3 position were designed, synthesized, characterized and screened through dilution method against a number of strains of bacteria including Streptococcus pneumonia, Staphylococcus aureus, Streptococcus pyogenes and Enterococcus which are either susceptible or resistant to erythromycin A. Results and Conclusion Preliminary antibacterial experiment showed that the 3 compounds had good antibacterial activity, especially ERY03 to erythromycin-resistant Streptococcus pneumonia.更多还原