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目的 寻找并合成抗耐药菌活性的 3位羟基红霉素衍生物。方法 以红霉素A为原料 ,经 9位酮基肟化 ,9位肟羟基 ,2′位羟基和 3′位二甲胺基同时苄基化 ,6位羟基甲基化 ,水解去 3位克拉定糖 ,氢化还原脱苄基 ,对甲基苄基或邻氯苄基取代 9位肟羟基等 6步反应 ,制得 3 羟基 6 O 甲基红霉素 9 肟基衍生物 ,其结构经1 3 CNMR ,FAB MS确证。结果 共制得 7个化合物 ,对其中 4个 (5 - 8)未见报道的化合物进行了体外抗菌活性测定。结论 5 ,7,8对部分红霉素诱导耐药菌有一定的活性
Objective To search and synthesize 3-hydroxy erythromycin derivatives with anti-drug-resistant activity. Methods Erythromycin A was used as the starting material. After 9-ketooximerization, 9-oxime hydroxyl, 2’-hydroxyl and 3’-dimethylamino were benzylated at the same time. 3-hydroxy 6-O-methylerythromycin 9 oxime derivatives were obtained by the reaction of 6-step reaction of 3-hydroxy-6-methylthiouracil, clavulactin, debenzylation by hydrogenation, p-methylbenzyl or o-chlorobenzyl, 1 3 CNMR, FAB MS confirmed. Results A total of seven compounds were prepared and the antibacterial activity of four compounds (5 - 8) were tested in vitro. Conclusion 5, 7, 8 to some erythromycin-resistant bacteria have some activity