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Trisubstituted Imidazoles as Mycobacterium tuberculosis Glutamine Synthetase Inhibitors
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
Uppsala University, Disciplinary Domain of Science and Technology, Biology, Department of Cell and Molecular Biology.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
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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
Abstract [en]

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.
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Medical and Health Sciences
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URN: urn:nbn:se:uu:diva-172589DOI: 10.1021/jm201212hISI: 000301767000031PubMedID: 22369127OAI: oai:DiVA.org:uu-172589DiVA: diva2:515127
Available from: 2012-04-12 Created: 2012-04-12 Last updated: 2017-12-07Bibliographically approved

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Gising, JohanNilsson, Mikael TOdell, Luke RLindh, MartinLarhed, MatsMowbray, Sherry LKarlén, Anders
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