NITD-916, a 4-hydroxy-2-pyridone derivative, is an orally active mycobacterial enoyl reductase InhA inhibitor with an IC 50 of 570 nM. NITD-916 forms a ternary complex with InhA and NADH to block access to the fatty acyl substrate binding pocket. NITD-916 inhibition of InhA reduces the synthesis of mycolic acids and results in cell death. NITD-916 has potent anti-tuberculosis effects.
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