KSK-104 has potent antibacterial activity against Mycobacterium tuberculosis ( MIC =0.78 μM). The role of KSK-104 is mainly involved in the synthesis and recovery pathways of pyridoxal 5'-phosphate (PLP), PLP-dependent enzymes and oxidative stress networks. KSK-104, as a candidate molecule for novel anti-tuberculosis drugs, can be used to develop research against drug-resistant mycobacterium tuberculosis.