@article{Campanico2019,
abstract = {Herein we report the screening of a small library of aurones and their isosteric counterparts, azaaurones and N‐acetylazaaurones, against Mycobacterium tuberculosis. Aurones were inactive at 20 µM, while azaurones and N‐acetylazaaurones emerged as the most potent compounds, with nine derivatives displaying MIC99 values ranging from 0.4 to 2.0 $\mu$M. In addition, several N‐acetylazaaurones were found to be active against multidrug resistant (MDR) and extensively drug resistant (XDR) clinical M. tuberculosis isolates. The anti‐mycobacterial mechanism of action of these compounds remains to be determined, however a preliminary mechanistic study confirmed that they do not inhibit the mycobacterial cytochrome bc1 complex. Additionally, microsomal metabolic stability and metabolite identification studies revealed that N‐acetylazaaurones are deacetylated to their azaaurone counterparts. Overall, these results demonstrate that azaaurones and their N‐acetyl counterparts represent a new entry in the toolbox of chemotypes capable of inhibiting M. tuberculosis growth.},
author = {Campani{\c{c}}o, Andre and Carrasco, Marta P and Njoroge, Mathew and Seldon, Ronnett and Chibale, Kelly and Perdig{\~{a}}o, Jo{\~{a}}o and Portugal, Isabel and Warner, Digby F and Moreira, Rui and Lopes, Francisca},
doi = {10.1002/cmdc.201900289},
file = {:C$\backslash$:/Users/01462563/AppData/Local/Mendeley Ltd./Mendeley Desktop/Downloaded/Campani{\c{c}}o et al. - 2019 - Azaaurones as potent antimycobacterial agents active against MDR‐ and XDR‐TB.pdf:pdf},
journal = {ChemMedChem},
keywords = {fund{\_}not{\_}ack,original},
mendeley-tags = {fund{\_}not{\_}ack,original},
month = {jul},
number = {16},
pages = {1537--1546},
publisher = {John Wiley {\&} Sons, Ltd},
title = {{Azaaurones as potent antimycobacterial agents active against MDR‐ and XDR‐TB}},
url = {https://onlinelibrary.wiley.com/doi/abs/10.1002/cmdc.201900289},
volume = {14},
year = {2019}
}

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The anti‐mycobacterial mechanism of action of these compounds remains to be determined, however a preliminary mechanistic study confirmed that they do not inhibit the mycobacterial cytochrome bc1 complex. Additionally, microsomal metabolic stability and metabolite identification studies revealed that N‐acetylazaaurones are deacetylated to their azaaurone counterparts. 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