Determination of relative affinity and inhibitory activity of pyrazolone analogs using Mycobacterium tuberculosis shikimate kinase LC-MS based screening assays

摘要

Tuberculosis is a worldwide pandemic and no new class of antituberculosis agents has been approved since the 1960s. Because shikimate kinase (SK) is an enzyme in the shikimate pathway essential for the growth of Mycobacterium tuberculosis (Mt) and not found in mammals, it is an attractive target for therapeutic intervention for tuberculosis (TB). The main aim of this study is to show the application of LC-MS based binding and functional assays to identify MtSK inhibitors from a series of pyrazolone analogs.