Acridones Are Highly Potent Inhibitors of Tachyzoites.
ACS Infectious Diseases
Acridone derivatives, which have been shown to have and activity against spp, inhibit proliferation at picomolar concentrations. Using enzymatic assays, we show that acridones inhibit both cytochrome and dihydroorotate dehydrogenase and identify acridones that bind preferentially to the Q site of cytochrome . We identify acridones that have efficacy in a murine model of systemic toxoplasmosis. Acridones have potent activity against and represent a promising new class of preclinical compounds.
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Alday, P. H., McConnell, E. V., Boitz Zarella, J. M., Dodean, R. A., Kancharla, P., Kelly, J. X., & Doggett, J. S. (2021). Acridones Are Highly Potent Inhibitors of Toxoplasma gondii Tachyzoites. ACS Infectious Diseases, acsinfecdis.1c00016. https://doi.org/10.1021/acsinfecdis.1c00016