新型单取代磺酰脲衍生物的合成与评价及其作为抗结核药物的研究。
Synthesis and evaluation of novel monosubstituted sulfonylurea derivatives as antituberculosis agents.
机构信息
State-Key Laboratory of Elemento-Organic Chemistry, National Pesticide Engineering Research Center(Tianjin), Nankai University, Tianjin 300071, China.
出版信息
Eur J Med Chem. 2012 Apr;50:18-26. doi: 10.1016/j.ejmech.2012.01.011. Epub 2012 Jan 15.
A series of novel monosubstituted sulfonylurea derivatives 10a-y were synthesized and characterized by (1)H NMR, (13)C NMR and HRMS. These compounds were evaluated against Mycobacterium tuberculosis H37Rv in vitro. The results showed compounds 10f, 10k and 10s exhibited moderate antituberculosis activities with MIC values in the range of 20-100 mg/L. Compounds 10b and 10o displayed good antituberculosis activities (MIC 10 mg/L), which were comparable with that of the sulfometuron methyl. Both of the two compounds showed little cytotoxicities, with an IC(50) against THP-1 cells greater than 100 mg/L.
一系列新型单取代磺酰脲衍生物 10a-y 通过 (1)H NMR、(13)C NMR 和高分辨质谱进行了合成和表征。这些化合物在体外针对结核分枝杆菌 H37Rv 进行了评估。结果表明，化合物 10f、10k 和 10s 具有中等的抗结核活性，MIC 值在 20-100mg/L 范围内。化合物 10b 和 10o 显示出良好的抗结核活性（MIC 10mg/L），与磺酰脲甲酯相当。这两个化合物的细胞毒性都很小，对 THP-1 细胞的 IC(50)大于 100mg/L。
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