Pyrazolo[1,5-a]pyridine-3-carboxamide hybrids: Design, synthesis and evaluation of anti-tubercular activity
Pyrazolo[1,5-a]pyridine-3-carboxamide hybrids: Design, synthesis and evaluation of anti-tubercular activity
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DOI：
10.1016/j.ejmech.2016.09.030
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发表时间：
2017-01-05
影响因子：
6.7
通讯作者：
Ding, Ke
中科院分区：
文献类型：
--
作者：
Lu, Xiaoyun;Tang, Jian;Ding, Ke
设计了一系列吡唑并[1,5-a]吡啶-3-甲酰胺杂化物并作为新型抗结核药物进行了评估。代表性杂交7对敏感菌株H37Rv和一组耐药Mtb菌株表现出良好的体外活性，MIC值分别为0.006μg/mL和0.003至0.014μg/mL。更重要的是，Hybrid 7还表现出非常低的细胞毒性，并且可以显着降低感染自发光H37Ra菌株的小鼠模型中的分枝杆菌负荷，这可能作为进一步开发新型抗结核药物的先导化合物。 (C) 2016 Elsevier Masson SAS。版权所有。
A series of pyrazolo[1,5-a]pyridine-3-carboxamide hybrids were designed and evaluated as novel anti tubercular agents. The representative hybrid 7 exhibited promising in vitro activity against susceptive Strain H37Rv and a panel of drug-resistant Mtb strains with MIC values of 0.006 mu g/mL and ranged from 0.003 to 0.014 mu g/mL, respectively. More importantly, the hybrid 7 also showed very low cytotoxicity, and could significantly reduce the mycobacterial burden in a mouse model infected with autoluminescent H37Ra strain, which may serve as a lead compound for further development of new anti-tubercular agents. (C) 2016 Elsevier Masson SAS. All rights reserved.