大环内酯类衍生物的合成及其体外抗菌活性  

Synthesis and antibacterial activities of new erythromycin derivatives

作　　者：冯润良[1] 宫平[1] 方林[1] 洪伟[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2004年第4期229-232,共4页Chinese Journal of Medicinal Chemistry

摘　　要：目的研究大环内酯类抗生素衍生物的合成及其抗菌活性。方法以红霉素为起始原料 ,经过肟化、重排和胺化反应合成目标化合物 ;测定目标化合物的抗菌活性。结果与结论设计、合成了10个红霉素衍生物 (YAM 1～YAM 10 ) ,所有化合物经质谱和核磁共振碳谱确证均为新化合物。化合物YAM 9的活性与红霉素相同 ,该化合物值得进一步研究。Aim To study the synthesis and antibacterial activity of macrolide derivatives.Methods Erythromycin derivatives were synthesized primarily from erythromycin via oximidation,rearrangement and amination reactions.The antibacterial activity of the ten compounds were tested.Results Ten compounds were synthesized (YAM-1～YAM-10 ).They were all novel compounds.The structures of the title compounds were identified by 13 C-NMR and MS spectrum analysis.Conclusion Compound YAM-9 showed antibacterial activity equivalent to that of erythromycin,and was recommended to further study.

关 键 词：药物化学 制备 化学合成 红霉素衍生物 抗菌活性 

分 类 号：R914[医药卫生—药物化学]