A Facile Hydroxyindole Carboxylic Acid Based Focused Library Approach for Potent and Selective Inhibitors of Mycobacterium Protein Tyrosine Phosphatase B. Issue 6 (8th April 2013)

• Record Type: Journal Article
• Authors: Zeng, Li‐Fan; Xu, Jie; He, Yantao; He, Rongjun; Wu, Li; Gunawan, Andrea M.; Zhang, Zhong‐Yin
• Is Part Of: ChemMedChem. Volume 8:Issue 6(2013:Jun.)
• Page Start: 904
• Page End: 908
• Publication Date: 2013-04-08
• Subjects: amides -- focused libraries -- inhibitors -- protein tyrosine phosphatases -- tuberculosis; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201300115
• Languages: English
• ISSNs: 1860-7179

Abstract

Abstract : Focused 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. Compound11 a shows high cellular activity and is capable of reversing the altered immune responses induced by mPTPB in macrophages.