Meng Qingyi, Luo Huibing, Chen Yilang, Wang Tiancai, Yao Qizheng
Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Bioorg Med Chem Lett. 2009 Sep 15;19(18):5372-5. doi: 10.1016/j.bmcl.2009.07.126. Epub 2009 Aug 6.
Guided by the metabolism information of SQ109, derivatives with substituted geranylamine moiety or substituted admantane ring of SQ109 were synthesized and evaluated as antituberculosis agents. Among all tested compounds, compound 11c showed the most potent antituberculosis activity with MIC value of 0.3 microM against Mycobacterium tuberculosis H37Rv.
以SQ109的代谢信息为指导，合成了具有取代香叶胺部分或取代金刚烷环的SQ109衍生物，并作为抗结核药物进行了评估。在所有测试的化合物中，化合物11c表现出最强的抗结核活性，对结核分枝杆菌H37Rv的MIC值为0.3微摩尔。
