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 μg/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.

中文翻译：

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作为抗结核剂的2-氯N-（4-（6-氯H-咪唑并[1,2-a]吡啶-2-基）苯基）乙酰胺衍生物的合成

本文报道了使用5-氯吡啶酮合成2-氯N-（4-（6-氯H-咪唑并[1,2 - a ]吡啶-2--2-基）苯基）乙酰胺衍生物（PINRAc 1-12）的方法。多步骤规程中的-2-胺和2-溴-1-（4-硝基苯基）乙酮。所有化合物的结构均通过NMR，FT-IR和GCMS表征。使用微孔板Alamar Blue测定法筛选化合物针对结核分枝杆菌H37Rv的抗结核活性。它们中的大多数在MIC范围为1.6–25μg/ mL时显示出良好的抗结核活性，对人胚胎肾细胞系进行的细胞毒性研究表明对正常细胞没有毒性。对接研究是针对来自苹果的霉菌酸转运蛋白MmpL3进行的。耻垢分枝杆菌支持了体外结果。