The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis

8-Nitro-benzothiazinones (BTZs), such as BTZ043 and PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro. Structure-activity relationship (SAR) studies revealed the 8-nitro group of the BTZ scaffol...

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Bibliografiske detaljer
Udgivet i:Antimicrob Agents Chemother
Main Authors: Makarov, Vadim, Neres, João, Hartkoorn, Ruben C., Ryabova, Olga B., Kazakova, Elena, Šarkan, Michal, Huszár, Stanislav, Piton, Jérémie, Kolly, Gaëlle S., Vocat, Anthony, Conroy, Trent M., Mikušová, Katarína, Cole, Stewart T.
Format: Artigo
Sprog:Inglês
Udgivet: American Society for Microbiology 2015
Fag:
Experimental Therapeutics
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4505264/
https://ncbi.nlm.nih.gov/pubmed/25987616
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1128/AAC.00778-15
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