大环内酯类9位羰基结构修饰衍生物的研究进展.PDF

PROGRESS IN PHARMACEUTICAL SCIENCES 2016,40 7 :535-541 ( ) 535 大环内酯类 9 位羰基结构修饰衍生物的研究进展 王绍菊，毕小玲 * （中国药科大学药物化学教研室，江苏 南京 210009） [ 摘要 ] 大环内酯类抗生素自上市以来一直用于治疗呼吸系统等疾病，但随着该类药物的广泛应用，耐药菌日益增多。为此，研究者们一 直致力于半合成大环内酯类抗生素的研究，希望开发出对耐药菌有效、抗菌谱广的半合成衍生物。综述近年来对大环内酯 9 位羰基结构 修饰的研究进展，并着重介绍一些活性较好的化合物。 [ 关键词 ] 红霉素；9 位结构修饰；肟醚；成环修饰；抗菌活性 [ 中图分类号 ] R978.15 [ 文献标志码 ] A [ 文章编号 ] 1001-5094（2016）07-0535-07 Progress in Macrolide Derivatives with C9- Carbonyl Modification WANG Shaoju, BI Xiaoling (Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China) [Abstract] Macrolide antibiotics have been used to treat respiratory and other infectious diseases since they were launched. However, their wide application have led to the increase in resistant strains of bacteria. Therefore, researchers have been concentrating on the investigation of semi-synthetic macrolide antibiotics, hoping to develop semi-synthetic derivatives with activity against resistant bacteria and broad antibacterial spectrum. The recent research progress in structure modification of C9-carbonyl of macrolide was reviewed, and some compounds with superior activity were highlighted as well. [Key words] erythromycin; C9-structure modification; oxime ether; ring modification; antibacterial activity 2 1 N N 红霉素（erythromycin， ）是最早用于临床的大环 HO HO