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Repositioning and Characterization of 1-(Pyridin-4-yl)pyrrolidin-2-one Derivatives as Plasmodium Cytoplasmic Prolyl-tRNA Synthetase Inhibitors

[Image: see text] Prolyl-tRNA synthetase (PRS) is a clinically validated antimalarial target. Screening of a set of PRS ATP-site binders, initially designed for human indications, led to identification of 1-(pyridin-4-yl)pyrrolidin-2-one derivatives representing a novel antimalarial scaffold. Eviden...

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Detalles Bibliográficos
Autores principales: Okaniwa, Masanori, Shibata, Akira, Ochida, Atsuko, Akao, Yuichiro, White, Karen L., Shackleford, David M., Duffy, Sandra, Lucantoni, Leonardo, Dey, Sumanta, Striepen, Josefine, Yeo, Tomas, Mok, Sachel, Aguiar, Anna Caroline C., Sturm, Angelika, Crespo, Benigno, Sanz, Laura M., Churchyard, Alisje, Baum, Jake, Pereira, Dhelio B., Guido, Rafael V. C., Dechering, Koen J., Wittlin, Sergio, Uhlemann, Anne-Catrin, Fidock, David A., Niles, Jacquin C., Avery, Vicky M., Charman, Susan A., Laleu, Benoît
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8204304/
https://www.ncbi.nlm.nih.gov/pubmed/33929818
http://dx.doi.org/10.1021/acsinfecdis.1c00020