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Molecules 2016, 21(1), 49; doi:10.3390/molecules21010049

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

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
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 2 November 2015 / Revised: 22 December 2015 / Accepted: 23 December 2015 / Published: 30 December 2015
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [890 KB, uploaded 30 December 2015]   |  

Abstract

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. View Full-Text
Keywords: imidazo[1,2-a]pyridine amide-cinnamamide hybrids; design; synthesis; antimycobacterial activity imidazo[1,2-a]pyridine amide-cinnamamide hybrids; design; synthesis; antimycobacterial activity
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Li, L.; Li, Z.; Liu, M.; Shen, W.; Wang, B.; Guo, H.; Lu, Y. Design, Synthesis and Antimycobacterial Activity of Novel Imidazo[1,2-a]pyridine Amide-Cinnamamide Hybrids. Molecules 2016, 21, 49.

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