Published on January 2022 | Medicinal Chemistry

Design, synthesis and anti-mycobacterial evaluation of imidazo[1,2-a]pyridine analogues

Based on the molecular hybridization strategy, thirty-four imidazo[1,2-a]pyridine amides (IPAs) and imidazo[1,2-a]pyridine sulfonamides (IPSs) were designed and synthesized. The structures of the target compounds were characterized using 1 H NMR, 13C NMR, LCMS, and elemental analyses. The synthesized compounds were evaluated in vitro for anti-tubercular activity using the microplate Alamar Blue assay against Mycobacterium tuberculosis H37Rv strain and the MIC was determined. The evaluated compounds exhibited MIC in the range 0.05–≤100 μg mL−1 . Among these derivatives, IPA-6 (MIC 0.05 μg mL−1 ), IPA-9 (MIC 0.4 μg mL−1 ), and IPS-1 (MIC 0.4 μg mL−1 ) displayed excellent anti-TB activity, whereas compounds IPA-5, IPA-7 and IPS-16 showed good anti-TB activity (MIC 0.8–3.12 μg mL−1 ). The most active compounds with MIC of