Importantly, THNA analogues 72 and 77 exhibited the best overall profiles, with potent MABA and LORA values (3–5 μg/mL) and no mammalian cytotoxicities (>32 μg/mL), reduced lipophilicity, improved hERG liability (1–13% inhibition of the hERG potassium channel at 1 μg/mL), shorter half-life (14–16 h vs 56 h for bedaquiline) and desirably faster clearance rate compared to the clinically-approved tuberculosis drug bedaquiline. This evidence concerns the gene KCNA3 and tuberculosis.