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SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF 3-HYDROXY-6-O-METHYLERYTHROMYCIN-9-O-SUBSTITUTED OXIME DERIVATIVES
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 8
- DOI:
- 10.3321/j.issn:0513-4870.2001.08.005
- Key Word:
- 3-羟基红霉素肟衍生物;半合成;抗菌活性
Abstract： 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13CNMR,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.
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