Rhodanine-Inspired Development of Dual-Action Mycobacterium tuberculosis Protein Tyrosine Phosphatase B Inhibitors

: 0.19 μM), good antituberculosis efficacy (MIC: 1.94 μg/mL), and high selectivity over human PTP1B (345-fold). It also demonstrated excellent metabolic stability, good permeability, acceptable bioavailability in mice, low cytotoxicity, and outperformed Rifampicin and Pretomanid in a macrophage infection model. Mechanistic studies showed that it reversed MptpB-mediated suppression of the macrophage MAPK pathway. This work validates the fusion strategy and identifies a promising lead targeting MptpB for further development.