Trisubstituted Imidazoles as Mycobacterium tuberculosis Glutamine Synthetase Inhibitors
2012 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 55, no 6, 2894-2898 p.Article in journal (Refereed) Published
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.
Place, publisher, year, edition, pages
2012. Vol. 55, no 6, 2894-2898 p.
Medical and Health Sciences
IdentifiersURN: urn:nbn:se:uu:diva-172589DOI: 10.1021/jm201212hISI: 000301767000031PubMedID: 22369127OAI: oai:DiVA.org:uu-172589DiVA: diva2:515127