A Facile Hydroxyindole Carboxylic Acid Based Focused Library Approach for Potent and Selective Inhibitors of Mycobacterium Protein Tyrosine Phosphatase B
Year: 2013
Type: article
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. Compound 11 a shows high cellular activity and is capable of reversing the altered immune responses induced by mPTPB in macrophages.
Source: ChemMedChem
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: green
OpenAlex ID: W2004278470