A facile hydroxyindole carboxylic acid based focused library approach for potent and selective inhibitors of Mycobacterium protein tyrosine phosphatase B

Zeng, Li-FanXu, JieHe, YantaoHe, RongjunWu, LiGunawan, Andrea M.Zhang, Zhong-Yin2025-05-122025-05-122013Zeng LF, Xu J, He Y, et al. A facile hydroxyindole carboxylic acid based focused library approach for potent and selective inhibitors of Mycobacterium protein tyrosine phosphatase B. ChemMedChem. 2013;8(6):904-908. doi:10.1002/cmdc.201300115https://hdl.handle.net/1805/47967Focused on Mtb: A facile hydroxyindole carboxylic acid based focused amide library was designed to target both the PTP active site and a unique nearby pocket for enhanced affinity and selectivity. HTS of the library led to the identification of a highly potent and selective inhibitor, 11 a, of mPTPB, an essential virulence factor for Mycobacterium tuberculosis. Compound 11 a shows high cellular activity and is capable of reversing the altered immune responses induced by mPTPB in macrophages.en-USPublisher PolicyFocused amide libraryHydroxyIndole carboxylic acidPTPmPTPB inhibitorTuberculosisA facile hydroxyindole carboxylic acid based focused library approach for potent and selective inhibitors of Mycobacterium protein tyrosine phosphatase BArticle