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Structure-Based Drug Design and Characterization of Sulfonyl-Piperazine Benzothiazinone Inhibitors of DprE1 from Mycobacterium tuberculosis

Macozinone (MCZ) is a tuberculosis (TB) drug candidate that specifically targets the essential flavoenzyme DprE1, thereby blocking synthesis of the cell wall precursor decaprenyl phosphoarabinose (DPA) and provoking lysis of Mycobacterium tuberculosis. As part of the MCZ backup program, we exploited...

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Detalles Bibliográficos
Autores principales: Piton, Jérémie, Vocat, Anthony, Lupien, Andréanne, Foo, Caroline S., Riabova, Olga, Makarov, Vadim, Cole, Stewart T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Society for Microbiology 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6153800/
https://www.ncbi.nlm.nih.gov/pubmed/30012754
http://dx.doi.org/10.1128/AAC.00681-18