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Trisubstituted Imidazoles as Mycobacterium tuberculosis Glutamine Synthetase Inhibitors†
[Image: see text] 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-...
| Autores principales: | , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical
Society
2012
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3381009/ https://www.ncbi.nlm.nih.gov/pubmed/22369127 http://dx.doi.org/10.1021/jm201212h |
| _version_ | 1782236362013933568 |
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| author | Gising, Johan Nilsson, Mikael T. Odell, Luke R. Yahiaoui, Samir Lindh, Martin Iyer, Harini Sinha, Achyut M. Srinivasa, Bachally R. Larhed, Mats Mowbray, Sherry L. Karlén, Anders |
| author_facet | Gising, Johan Nilsson, Mikael T. Odell, Luke R. Yahiaoui, Samir Lindh, Martin Iyer, Harini Sinha, Achyut M. Srinivasa, Bachally R. Larhed, Mats Mowbray, Sherry L. Karlén, Anders |
| author_sort | Gising, Johan |
| collection | PubMed |
| description | [Image: see text] 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. |
| format | Online Article Text |
| id | pubmed-3381009 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2012 |
| publisher | American Chemical
Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-33810092012-06-25 Trisubstituted Imidazoles as Mycobacterium tuberculosis Glutamine Synthetase Inhibitors† Gising, Johan Nilsson, Mikael T. Odell, Luke R. Yahiaoui, Samir Lindh, Martin Iyer, Harini Sinha, Achyut M. Srinivasa, Bachally R. Larhed, Mats Mowbray, Sherry L. Karlén, Anders J Med Chem [Image: see text] 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. American Chemical Society 2012-02-27 2012-03-22 /pmc/articles/PMC3381009/ /pubmed/22369127 http://dx.doi.org/10.1021/jm201212h Text en Copyright © 2012 American Chemical Society http://pubs.acs.org This is an open-access article distributed under the ACS AuthorChoice Terms & Conditions. Any use of this article, must conform to the terms of that license which are available at http://pubs.acs.org. |
| spellingShingle | Gising, Johan Nilsson, Mikael T. Odell, Luke R. Yahiaoui, Samir Lindh, Martin Iyer, Harini Sinha, Achyut M. Srinivasa, Bachally R. Larhed, Mats Mowbray, Sherry L. Karlén, Anders Trisubstituted Imidazoles as Mycobacterium tuberculosis Glutamine Synthetase Inhibitors† |
| title | Trisubstituted Imidazoles
as Mycobacterium tuberculosis Glutamine Synthetase
Inhibitors† |
| title_full | Trisubstituted Imidazoles
as Mycobacterium tuberculosis Glutamine Synthetase
Inhibitors† |
| title_fullStr | Trisubstituted Imidazoles
as Mycobacterium tuberculosis Glutamine Synthetase
Inhibitors† |
| title_full_unstemmed | Trisubstituted Imidazoles
as Mycobacterium tuberculosis Glutamine Synthetase
Inhibitors† |
| title_short | Trisubstituted Imidazoles
as Mycobacterium tuberculosis Glutamine Synthetase
Inhibitors† |
| title_sort | trisubstituted imidazoles
as mycobacterium tuberculosis glutamine synthetase
inhibitors† |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3381009/ https://www.ncbi.nlm.nih.gov/pubmed/22369127 http://dx.doi.org/10.1021/jm201212h |
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