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dc.contributor.authorSonopo, Molahlehi S.
dc.contributor.authorZeevaart, Jan R.
dc.contributor.authorPillay, Adushan
dc.contributor.authorChibale, Kelly
dc.contributor.authorMarjanovic-Painter, Biljana
dc.date.accessioned2017-03-14T06:18:11Z
dc.date.available2017-03-14T06:18:11Z
dc.date.issued2016
dc.identifier.citationSonopo, M.S. et al. 2016. Carbon‐14 radiolabeling and tissue distribution evaluation of MMV390048. Journal of labelled compounds and radiopharmaceuticals, 59(14):680-688. Special issue: 12th International Isotope Symposium on the Synthesis and Applications of Isotopes and Isotopically Labelled Compounds (IIS), 7-11 Jun 2015, Princeton, NJ. [https://doi.org/10.1002/jlcr.3445]en_US
dc.identifier.issn0362-4803
dc.identifier.issn1099-1344 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/20805
dc.identifier.urihttps://onlinelibrary.wiley.com/doi/abs/10.1002/jlcr.3445
dc.identifier.urihttps://doi.org/10.1002/jlcr.3445
dc.description.abstractThe antimalarial compound MMV390048 ([14C]-11) was labeled with carbon-14 isotope via a 3-step synthesis. It was obtained in a 15.5% radiochemical overall yield from carbon-14 labeled methyl iodide with a radiochemical purity of >99%. After single oral administration of [14C]-11 to albino and pigmented rats its tissue distribution profile was studied. Tissue distribution results showed high local exposure in the GI tract and excretory organs but low exposure of all other tissues. The radioactivity uptake was higher in the eyes of the pigmented rats than in the eyes of the albino rats at all-time points. The highest accumulation reached in the eyes of the pigmented rats was 0.46% at 6 hours. However, these levels are still very low as compared to the other organs studied. There was very little radioactivity from MMV390048 ([14C]-11) present in the skin of both the albino and pigmented rats. The results obtained are supportive of further development of MMV390048 as a potential antimalarial compounden_US
dc.language.isoenen_US
dc.publisherWileyen_US
dc.subjectAminopyridineen_US
dc.subjectAntimalarial agenten_US
dc.subjectCarbon‐14en_US
dc.subjectPlasmodium falciparumen_US
dc.subjectTissue distributionen_US
dc.titleCarbon‐14 radiolabeling and tissue distribution evaluation of MMV390048en_US
dc.typePresentationen_US
dc.contributor.researchID16951484 - Zeevaart, Jan Rijn


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