Novel inhibitors of Plasmodium Phosphatidylinositol 4-kinase IIIβ with low propensity for resistance : life cycle stage activity and in vivo efficacy in a humanized mouse malaria infection model
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Publisher
American Chemical Society
Abstract
Please read abstract in the article.
Description
SUPPORTING INFORMATION 1. Synthesis of intermediates; analytical spectra of compounds profiled in vivo; parasitology methods; PvPI4K and human kinase assays; in vitro ADME assays, and mouse pharmacokinetic and in vivo efficacy studies (PDF).
SUPPORTING INFORMATION 2. In vitro data of all final compounds (mean IC50 values ± standard deviation (SD) or standard error (SE)) (CSV).
SUPPORTING INFORMATION 3. Molecular formula strings (CSV).
Keywords
Assays, Inhibition, Parasites, Photovoltaics, Rodent models, Ataxia-telangiectasia-mutated (ATM), Artemisinin-based combination therapy (ACT), Malaria, Seasonal malaria chemoprevention (SMC)
Sustainable Development Goals
SDG-03: Good health and well-being
Citation
Dziwornu, G.A., Mmonwa, M.M., Coertzen, D. et al. 2025, 'Novel inhibitors of Plasmodium Phosphatidylinositol 4-kinase IIIβ with low propensity for resistance: life cycle stage activity and in vivo efficacy in a humanized mouse malaria infection model', Journal of Medicinal Chemistry, vol. 68, no. 16, pp. 17736–17751, doi : 10.1021/acs.jmedchem.5c01417.