Synthesis of 2-Chloro-N-(4-(6-chloroH-imidazo[1,2-a]pyridin-2-yl)phenyl ) Acetamide Derivatives as Antitubercular Agents

AfraQuasar A. Nadaf, Supreet Gaonkar,Shivaraj Mantur, Mahesh S. Najare,Mohammed Yaseen, Manjunath G. Sunagar,Shrinivas Joshi,Imtiyaz Ahmed M. Khazi

CHEMISTRYSELECT(2020)

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Abstract
The present article reports the synthesis of 2-chloro-N-(4-(6-chloroH-imidazo[1,2-a]pyridin-2-yl)phenyl)acetamide derivatives (PINRAc 1-12) using 5-chloropyridin-2-amine and 2-bromo-1-(4-nitrophenyl)ethanone in a multi-step protocol. The structures of all the compounds were characterized by NMR, FT-IR and GCMS. The compounds were screened for their antitubercular activity against Mycobacterium tuberculosis H37Rv using the microplate Alamar Blue assay. Most of them exhibited good antitubercular activity with MIC in the range of 1.6-25 mu g/mL and the cytotoxicity study carried out on human embryonic kidney cell line showed no toxicity on the normal cells. The docking study was performed on mycolic acid transporter protein MmpL3 from Mycobacterium smegmatis which supported the in vitro results.
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Key words
Antitubercular activity,Biological Activity,Cytotoxicity,MmpL3,Mycobacterium tuberculosis H37RV,2-chloro-N-(4-(6-chloroH-imidazo[1,2-a]pyridin-2-yl)phenyl)acetamide
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