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Synthesis of Deuterated Endochin‐Like Quinolones

https://doi.org/10.1002/jlcr.4092

Pou, Sovitj ; Winter, Rolf W. ; Liebman, Katherine M. ; Dodean, Rosie A. ; Nilsen, Aaron ; DeBarber, Andrea ; Doggett, J. Stone ; Riscoe, Michael K. ( April 2024 , Journal of Labelled Compounds and Radiopharmaceuticals)

ABSTRACT
Malaria continues to be a serious and debilitating disease. The emergence and spread of high‐level resistance to multiple antimalarial drugs byPlasmodium falciparumhas brought about an urgent need for new treatments that will be active against multidrug resistant malaria infections. One such treatment,ELQ‐331(MMV‐167), an alkoxy carbonate prodrug of 4(1H)‐quinoloneELQ‐300, is currently in preclinical development with the Medicines for Malaria Venture. Clinical development ofELQ‐331or similar compounds will require the availability of isotopically labeled analogs. Unfortunately, a suitable method for the deuteration of these important compounds was not found in the literature. Here, we describe a facile and scalable method for the deuteration of 4(1H)‐quinoloneELQ‐300, its alkoxycarbonate prodrugELQ‐331, and their respective N‐oxides using deuterated acetic acid.

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Acridones Are Highly Potent Inhibitors of Toxoplasma gondii Tachyzoites

https://doi.org/10.1021/acsinfecdis.1c00016

Alday, P. Holland ; McConnell, Erin V. ; Boitz Zarella, Jan M. ; Dodean, Rozalia A. ; Kancharla, Papireddy ; Kelly, Jane X. ; Doggett, J. Stone ( July 2021 , ACS Infectious Diseases)
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Antimalarial proteasome inhibitor reveals collateral sensitivity from intersubunit interactions and fitness cost of resistance

https://doi.org/10.1073/pnas.1806109115

Kirkman, Laura A. ; Zhan, Wenhu ; Visone, Joseph ; Dziedziech, Alexis ; Singh, Pradeep K. ; Fan, Hao ; Tong, Xinran ; Bruzual, Igor ; Hara, Ryoma ; Kawasaki, Masanori ; et al ( July 2018 , Proceedings of the National Academy of Sciences)