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Mt KARI-IN-5 (compound 6c) was a potent inhibitor of Mycobacterium tuberculosis ketohydrin reductase I (MtbKARI) (Ki: 4.72 μM). Mt KARI-IN-5 exhibited inhibition of MtbH37Rv activity with a MIC value of 1.56 μM, low cytotoxicity and an IC50 value for HEK The IC50 value for HEK was greater than 64 μg/mL.