High-throughput discovery of mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) inhibitors using click chemistry

Abstract

A ∼500-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 i as low as 150 nM) and selective MptpB inhibitors, some of which represent the most potent MptpB inhibitors developed to date. © 2009 American Chemical society.