National Center for
3ZXR: Crystal Structure Of Mycobacterium Tuberculosis Glutamine Synthetase In Complex With Tri-Substituted Imidazole Inhibitor (3-(2-Tert-Butyl-5-(Pyridin-4-Yl)-1h-Imidazol-4-Yl)quinoline) And L-Methionine-S-Sulfoximine Phosphate
J. Med. Chem. (2012) 55 p.2894-2898» All references (3)
Mycobacterium tuberculosis glutamine synthetase (MtGS) is a promising target for antituberculosis drug discovery. In a recent high-throughput screening study we identified several classes of MtGS inhibitors targeting the ATP-binding site. We now explore one of these classes, the 2-tert-butyl-4,5-diarylimidazoles, and present the design, synthesis, and X-ray crystallographic studies leading to the identification of MtGS inhibitors with submicromolar IC(50) values and promising antituberculosis MIC values.