High-Throughput Discovery of Mycobacterium tuberculosis Protein Tyrosine Phosphatase B (MptpB) Inhibitors Using Click Chemistry

A similar to 3500-member library of bidentate inhibitors against protein tyrosine phosphatases (PTPs) was rapidly assembled using click chemistry. Subsequent high-throughput screening had led to the discovery of highly potent (K-1 as low as 150 nM) and selective MptpB inhibitors, some of which represent the most potent MptpB inhibitors developed to date.