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.