Li Linhu, Li Zhuorong, Liu Mingliang, Shen Weiyi, Wang Bin, Guo Huiyuan, Lu Yu
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Zhejiang Starry Pharmaceutical Co. Ltd., Xianju 317300, China.
Molecules. 2015 Dec 30;21(1):E49. doi: 10.3390/molecules21010049.
We report herein the design and synthesis of a series of novel imidazo[1,2-a]pyridine amide-cinnamamide hybrids linked via an alkyl carbon chain. All 38 new hybrids were evaluated for their antimycobacterial activity against M. tuberculosis (MTB) H37Rv ATCC 27294 using the microplate Alamar Blue assay (MABA). Although the hybrids are less active than the two reference compounds, the promising activity (MICs: 4 μg/mL) of 2,6-dimethylimidazo[1,2-a]pyridine amide-cinnamamide hybrids 11e and 11k could be a good starting point to further find new lead compounds against multi-drug-resistant tuberculosis.
我们在此报告了一系列通过烷基碳链连接的新型咪唑并[1,2-a]吡啶酰胺-肉桂酰胺杂化物的设计与合成。使用微孔板Alamar蓝分析法(MABA)对所有38种新杂化物针对结核分枝杆菌(MTB)H37Rv ATCC 27294的抗分枝杆菌活性进行了评估。尽管这些杂化物的活性低于两种参考化合物,但2,6-二甲基咪唑并[1,2-a]吡啶酰胺-肉桂酰胺杂化物11e和11k的有前景的活性(最低抑菌浓度:4μg/mL)可能是进一步寻找抗多药耐药结核病新先导化合物的良好起点。