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Carbon‐14 radiolabeling and tissue distribution evaluation of MMV390048
Author(s) -
Sonopo Molahlehi S.,
Pillay Adushan,
Chibale Kelly,
MarjanovicPainter Biljana,
Donini Cristina,
Zeevaart Jan R.
Publication year - 2016
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3445
Subject(s) - chemistry , carbon 14 , methyl iodide , isotopes of carbon , distribution (mathematics) , excretory system , tissue distribution , iodide , radiochemistry , pharmacology , endocrinology , medicine , organic chemistry , total organic carbon , mathematical analysis , physics , mathematics , quantum mechanics
The antimalarial compound MMV390048 ( [ 14 C ]‐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 [ 14 C ]‐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 ( [ 14 C ]‐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 compound.