发现具有抗结核分枝杆菌 H37Rv 活性的新型 1,3,5-三嗪支架。
Discovery of new 1,3,5-triazine scaffolds with potent activity against Mycobacterium tuberculosis H37Rv.
机构信息
Medicinal and Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow 226001, India.
出版信息
Eur J Med Chem. 2010 Aug;45(8):3335-45. doi: 10.1016/j.ejmech.2010.04.017. Epub 2010 Apr 20.
A series of eighty one 2,4,6-trisubstituted-1,3,5-triazines were synthesized and evaluated in vitro for the growth inhibition of Mycobacterium tuberculosis H37Rv. Fifteen compounds from this series exhibited good to moderate activity with an MIC in the range 1.56-3.12 microg/mL and most of them were found to be nontoxic against VERO cells and MBMDMQs (mouse bone marrow derived macrophages). This is for the first time that 2,4,6-trisubstituted-1,3,5-triazines were identified as a potent inhibitors of M. tuberculosis H37Rv.
合成了一系列 81 种 2,4,6-三取代-1,3,5-三嗪，并对其体外抑制分枝杆菌 H37Rv 的生长进行了评价。该系列中有 15 种化合物表现出良好至中等的活性，MIC 范围为 1.56-3.12μg/mL，其中大多数对 VERO 细胞和 MBMDMQs（鼠骨髓来源的巨噬细胞）无毒性。这是首次发现 2,4,6-三取代-1,3,5-三嗪是分枝杆菌 H37Rv 的有效抑制剂。
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