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Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays.


ABSTRACT: Small-molecule inhibitors of the mycobacterial transcriptional repressor EthR have previously been shown to act as boosters of the second-line antituberculosis drug ethionamide. Fragment-based drug discovery approaches have been used in the past to make highly potent EthR inhibitors with ethionamide boosting activity both in vitro and ex vivo. Herein, we report the development of fragment-sized EthR ligands with nanomolar minimum effective concentration values for boosting the ethionamide activity in Mycobacterium tuberculosis whole-cell assays.

SUBMITTER: Nikiforov PO 

PROVIDER: S-EPMC5474694 | biostudies-literature | 2017 May

REPOSITORIES: biostudies-literature

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Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays.

Nikiforov Petar O PO   Blaszczyk Michal M   Surade Sachin S   Boshoff Helena I HI   Sajid Andaleeb A   Delorme Vincent V   Deboosere Nathalie N   Brodin Priscille P   Baulard Alain R AR   Barry Clifton E CE   Blundell Tom L TL   Abell Chris C  

ACS chemical biology 20170405 5


Small-molecule inhibitors of the mycobacterial transcriptional repressor EthR have previously been shown to act as boosters of the second-line antituberculosis drug ethionamide. Fragment-based drug discovery approaches have been used in the past to make highly potent EthR inhibitors with ethionamide boosting activity both in vitro and ex vivo. Herein, we report the development of fragment-sized EthR ligands with nanomolar minimum effective concentration values for boosting the ethionamide activi  ...[more]

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