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Optimization and Evaluation of 5-Styryl-Oxathiazol-2-one Mycobacterium tuberculosis Proteasome Inhibitors as Potential Antitubercular Agents
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.
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, Structure and Molecular Biology. Uppsala University, Science for Life Laboratory, SciLifeLab.
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2015 (English)In: ChemistryOpen, ISSN 2191-1363, Vol. 4, no 3, 342-362 p.Article in journal (Refereed) Published
Abstract [en]

This is the first report of 5-styryl-oxathiazol-2-ones as inhibitors of the Mycobacterium tuberculosis (Mtb) proteasome. As part of the study, the structure-activity relationship of oxathiazolones as Mtb proteasome inhibitors has been investigated. Furthermore, the prepared compounds displayed a good selectivity profile for Mtb compared to the human proteasome. The 5-styryl-oxathiazol-2-one inhibitors identified showed little activity against replicating Mtb, but were rapidly bactericidal against nonreplicating bacteria. (E)-5-(4-Chlorostyryl)-1,3,4-oxathiazol-2-one) was most effective, reducing the colony-forming units (CFU)/mL below the detection limit in only seven days at all concentrations tested. The results suggest that this new class of Mtb proteasome inhibitors has the potential to be further developed into novel antitubercular agents for synergistic combination therapies with existing drugs.

Place, publisher, year, edition, pages
2015. Vol. 4, no 3, 342-362 p.
Keyword [en]
antitubercular agents, 5-styryl-oxathiazolones, Mtb proteasome inhibitor, Mycobacterium tuberculosis, nonreplicating Mtb, rapid bactericidal activity
National Category
Chemical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-258781DOI: 10.1002/open.201500001ISI: 000356820900015OAI: oai:DiVA.org:uu-258781DiVA: diva2:842406
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VINNOVA
Available from: 2015-07-20 Created: 2015-07-20 Last updated: 2017-12-04Bibliographically approved

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Gising, JohanÅkerbladh, LindaRoos, Annette K.Mowbray, Sherry L.Karlén, AndersLarhed, Mats

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Organic Pharmaceutical ChemistryStructure and Molecular BiologyScience for Life Laboratory, SciLifeLabDepartment of Cell and Molecular Biology
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