2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1.

doi:10.1021/cb5007163

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Article

2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1.

ACS chemical biology - 20 Mar 2015

Neres João, Hartkoorn Ruben C, Chiarelli Laurent R, Gadupudi Ramakrishna, Pasca Maria Rosalia, Mori Giorgia, Venturelli Alberto, Savina Svetlana, Makarov Vadim, Kolly Gaelle S, Molteni Elisabetta, Binda Claudia, Dhar Neeraj, Ferrari Stefania, Brodin Priscille, Delorme Vincent, Landry Valérie, de Jesus Lopes Ribeiro Ana Luisa, Farina Davide, Saxena Puneet, Pojer Florence, Carta Antonio, Luciani Rosaria, Porta Alessio, Zanoni Giuseppe, De Rossi Edda, Costi Maria Paola, Riccardi Giovanna, Cole Stewart T

Abstract excerpt

Phenotypic screening of a quinoxaline library against replicating Mycobacterium tuberculosis led to the identification of lead compound Ty38c (3-((4-methoxybenzyl)amino)-6-(trifluoromethyl)quinoxaline-2-carboxylic acid). With an MIC99 and MBC of 3.1 μM, Ty38c is bactericidal and active against intracellular bacteria. To investigate its mechanism of action, we isolated mutants resistant to Ty38c and sequenced...

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PMID: 25427196
DOI: 10.1021/cb5007163

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