William Nguyen, Coralie Boulet, Madeline G Dans, Katie Loi, Kate E Jarman, Gabrielle M Watson, Wai-Hong Tham, Kate J Fairhurst, Tomas Yeo, David A Fidock, Sergio Wittlin, Mrittika Chowdury, Tania F de Koning-Ward, Gong Chen, Dandan Yan, Susan A Charman, Delphine Baud, Stephen Brand, Paul F Jackson, Alan F Cowman, Paul R Gilson, Brad E Sleebs
Malaria is a devastating disease that causes significant morbidity worldwide. The development of new antimalarial chemotypes is urgently needed because of the emergence of resistance to frontline therapies. Independent phenotypic screening campaigns against the Plasmodium asexual parasite, including our own, identified the aryl amino acetamide hit scaffold. In a prior study, we identified the STAR-related lipid transfer protein (PfSTART1) as the molecular target of this antimalarial chemotype. In this study, we combined structural elements from the different aryl acetamide hit subtypes and explored the structure-activity relationship...
March 25, 2024: European Journal of Medicinal Chemistry