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Okaniwa, M.; Shibata, A.; Ochida, A.; Akao, Y.; White, K. L.; Shackleford, D. M.; Duffy, S.; Lucantoni, L.; Dey, S.; Striepen, J.; Yeo, T.; Mok, S.; Aguiar, A. C. C.; Sturm, A.; Crespo, B.; Sanz, L. M.; Churchyard, A.; Baum, J.; Pereira, D. B.; Guido, R. V. C.; Dechering, K. J.; Wittlin, S.; Uhlemann, A. C.; Fidock, D. A.; Niles, J. C.; Avery, V. M.; Charman, S. A.; Laleu, B.
2021
Repositioning and characterization of 1-(pyridin-4-yl)pyrrolidin-2-one derivatives as Plasmodium cytoplasmic prolyl-trna synthetase inhibitors
Cheuka, P. M.; Centani, L.; Arendse, L. B.; Fienberg, S.; Wambua, L.; Renga, S. S.; Dziwornu, G. A.; Kumar, M.; Lawrence, N.; Taylor, D.; Wittlin, S.; Coertzen, D.; Reader, J.; van der Watt, M.; Birkholtz, L. M.; Chibale, K.
2021
New amidated 3,6-diphenylated imidazopyridazines with potent antiplasmodium activity are dual inhibitors of; Plasmodium; phosphatidylinositol-4-kinase and cGMP-dependent protein kinase
Xie, S. C.; Metcalfe, R. D.; Mizutani, H.; Puhalovich, T.; Hanssen, E.; Morton, C. J.; Du, Y.; Dogovski, C.; Huang, S. C.; Ciavarri, J.; Hales, P.; Griffin, R. J.; Cohen, L. H.; Chuang, B. C.; Wittlin, S.; Deni, I.; Yeo, T.; Ward, K. E.; Barry, D. C.; Liu, B.; Gillett, D. L.; Crespo-Fernandez, B. F.; Ottilie, S.; Mittal, N.; Churchyard, A.; Ferguson, D.; Aguiar, A. C. C.; Guido, R. V. C.; Baum, J.; Hanson, K. K.; Winzeler, E. A.; Gamo, F. J.; Fidock, D. A.; Baud, D.; Parker, M. W.; Brand, S.; Dick, L. R.; Griffin, M. D. W.; Gould, A. E.; Tilley, L.
2021
Design of proteasome inhibitors with oral efficacy in vivo against Plasmodium falciparum and selectivity over the human proteasome
Horatscheck, A.; Andrijevic, A.; Nchinda, A. T.; Le Manach, C.; Paquet, T.; Khonde, L. P.; Dam, J.; Pawar, K.; Taylor, D.; Lawrence, N.; Brunschwig, C.; Gibhard, L.; Njoroge, M.; Reader, J.; van der Watt, M.; Wicht, K.; de Sousa, A. C. C.; Okombo, J.; Maepa, K.; Egan, T. J.; Birkholtz, L. M.; Basarab, G. S.; Wittlin, S.; Fish, P. V.; Street, L. J.; Duffy, J.; Chibale, K.
2020
Identification of 2,4-disubstituted imidazopyridines as hemozoin formation inhibitors with fast-killing kinetics and in vivo efficacy in the Plasmodium falciparum NSG mouse model
Antimalarial pyrido[1,2-a]benzimidazole derivatives with mannich base side chains: synthesis, pharmacological evaluation and reactive metabolite trapping studies
Gilson, Paul R.; Nguyen, William; Poole, William A.; Teixeira, Jose E.; Thompson, Jennifer K.; Guo, Kaiyuan; Stewart, Rebecca J.; Ashton, Trent D.; White, Karen L.; Sanz, Laura M.; Gamo, Francisco-Javier; Charman, Susan A.; Wittlin, Sergio; Duffy, James; Tonkin, Christopher J.; Tham, Wai-Hong; Crabb, Brendan S.; Cooke, Brian M.; Huston, Christopher D.; Cowman, Alan F.; Sleebs, Brad E.
2019
Evaluation of 4-Amino 2-Anilinoquinazolines against Plasmodium and Other Evaluation of 4-amino 2-anilinoquinazolines against Plasmodium and other apicomplexan parasites in vitro and in a P. falciparum humanized NOD-scid IL2Rynull mouse model of malaria
Schalkwijk, Joost; Allman, Erik L.; Jansen, Patrick A. M.; de Vries, Laura E.; Verhoef, Julie M. J.; Jackowski, Suzanne; Botman, Peter N. M.; Beuckens-Schortinghuis, Christien A.; Koolen, Karin M. J.; Bolscher, Judith M.; Vos, Martijn W.; Miller, Karen; Reeves, Stacy A.; Pett, Helmi; Trevitt, Graham; Wittlin, Sergio; Scheurer, Christian; Sax, Sibylle; Fischli, Christoph; Angulo-Barturen, Iñigo; Jiménez-Diaz, Mariá Belén; Josling, Gabrielle; Kooij, Taco W. A.; Bonnert, Roger; Campo, Brice; Blaauw, Richard H.; Rutjes, Floris P. J. T.; Sauerwein, Robert W.; Llinás, Manuel; Hermkens, Pedro H. H.; Dechering, Koen J.
2019
Antimalarial pantothenamide metabolites target acetyl-coenzyme A biosynthesis in Plasmodium falciparum