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Karale, Uttam B; Shinde, Akash U; Babar, Dattatraya A; Sangu, Komal G; Vagolu, Siva Krishna; Eruva, Vamshi K; Jadav, Surender S; Misra, Sunil; Dharmarajan, Sriram; Rode, Haridas B
Archiv der Pharmazie (Weinheim), 10/2021, Volume: 354, Issue: 10Journal Article
Novel inhibitors are needed to tackle tuberculosis. Herein, we report the 3‐aryl‐substituted imidazo1,2‐apyridines as potent antituberculosis agents. A small library of 3‐aryl‐substituted imidazo1,2‐apyridines 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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