Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids

被引：20
作者：
Li, Linhu [1 ,2 ]
Li, Zhuorong [1 ,2 ]
Liu, Mingliang [1 ,2 ]
Shen, Weiyi
Wang, Bin [3 ,4 ]
Guo, Huiyuan [1 ,2 ]
Lu, Yu [3 ,4 ]
机构：
[1] Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China
[2] Peking Union Med Coll, Beijing 100050, Peoples R China
[3] Zhejiang Starry Pharmaceut Co Ltd, Xianju 317300, Peoples R China
[4] Capital Med Univ, Beijing Key Lab Drug Resistance TB Res, Beijing TB & Thorac Tumor Res Inst, Dept Pharmacol,Beijing Chest Hosp, Beijing 101149, Peoples R China
来源：
MOLECULES | 2016年 / 21卷 / 01期
关键词：
imidazo[1; 2-a]pyridine amide-cinnamamide hybrids; design; synthesis; antimycobacterial activity; CINNAMIC ACID-DERIVATIVES; CLINICAL CANDIDATE; TUBERCULOSIS; OPTIMIZATION; SERIES; AGENTS; Q203;
D O I：
10.3390/molecules21010049
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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 g/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.
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页数：14
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