Citation: Li Linhu, Wang Apeng, Wang Bin, Liu Mingliang, Lv Kai, Tao Zeyu, Ma Chao, Ma Xican, Han Bing, Wang Aoyu, Lu Yu. N-(2-Phenoxy)ethyl imidazo[1, 2-a]pyridine-3-carboxamides containing various amine moieties: Design, synthesis and antitubercular activity[J]. Chinese Chemical Letters, ;2020, 31(2): 409-412. doi: 10.1016/j.cclet.2019.07.038 shu

N-(2-Phenoxy)ethyl imidazo[1, 2-a]pyridine-3-carboxamides containing various amine moieties: Design, synthesis and antitubercular activity

Li Linhu ^a,b,1 ,
Wang Apeng ^a,1 ,
Wang Bin ^c ,
Liu Mingliang ^a,*, ,
Lv Kai ^a ,
Tao Zeyu ^a ,
Ma Chao ^a ,
Ma Xican ^a ,
Han Bing ^a ,
Wang Aoyu ^a ,
Lu Yu ^c,*,

a.
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
b.
Limin Chemical Co., Ltd., Xinyi 221422, China
c.
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 100149, China

lmllyx@126.com

luyu4876@hotmail.com

Received Date: 22 June 2019
Revised Date: 12 July 2019
Accepted Date: 16 July 2019
Available Online: 17 July 2019

Figures(2)

Seven 2, 6-disubstituted N-(2-phenoxy)ethyl imidazo[1, 2-a]pyridine-3-carboxamide series containing various amine moieties were designed and synthesized as new anti-TB agents. Many of them show excellent in vitro activity against both drug-sensitive MTB strain H37Rv and two MDR-MTB clinical isolates (MIC: < 0.002-0.030 μg/mL). Compounds 2f, 5e and 5g display acceptable safety and pharmacokinetic profiles, opening a new direction for further development.
- N-(2-Phenoxy)ethyl imidazo[1, 2-a]pyridine,
- Design,
- Synthesis,
- Antimycobacterial activity
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