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  • Title: 3-Aryl-substituted imidazo[1,2-a]pyridines as antituberculosis agents.
    Author: Karale UB, Shinde AU, Babar DA, Sangu KG, Vagolu SK, Eruva VK, Jadav SS, Misra S, Dharmarajan S, Rode HB.
    Journal: Arch Pharm (Weinheim); 2021 Oct; 354(10):e2000419. PubMed ID: 34185337.
    Abstract:
    Novel inhibitors are needed to tackle tuberculosis. Herein, we report the 3-aryl-substituted imidazo[1,2-a]pyridines as potent antituberculosis agents. A small library of 3-aryl-substituted imidazo[1,2-a]pyridines was synthesized using direct arylation, followed by nitro reduction and finally Pd-catalyzed C-N coupling reactions. The compounds thus obtained were evaluated against Mycobacterium tuberculosis H37Rv. Compound 26 was identified as an antituberculosis lead with a minimum inhibitory concentration of 2.3 μg/ml against M. tuberculosis H37Rv. This compound showed a selectivity index of 35. The docking of 26 in the active site of the M. tuberculosis cytochrome bc1 complex cytochrome b subunit (Mtb QcrB) revealed key π-π interactions of compound 26 with the Tyr389 and Trp312 residues of Mtb QcrB.
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