SMARt751 targets the transcriptional regulatory factor VirS, inhibits its DNA binding ability, upregulates the mymA operon expression, thereby activating Ethionamide , enhancing the antimicrobial activity of Ethionamide. SMARt751 enhances the antibacterial activity of Ethionamide against M. tuberculosis, reverses the Ethionamide resistance. SMARt751 improves the antibacterial effect of Ethionamide and reduces its effective dose in mouse models. SMARt751 can cross blood brain barrier[1].