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

Molecules

Linhu Li¹  Zhuorong Li¹  Mingliang Liu¹  Weiyi Shen²  Bin Wang³  Huiyuan Guo¹  Yu Lu³ 

[1]Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China

[2]Zhejiang Starry Pharmaceutical Co. Ltd., Xianju 317300, China

[3]Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital Medical University, Beijing 101149, China

关键词: imidazo[1;    2-a]pyridine amide-cinnamamide hybrids;    design;    synthesis;    antimycobacterial activity;   

DOI  :  10.3390/molecules21010049

来源: mdpi

【 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 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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.