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Carbon‐14 radiolabelling and tissue distribution evaluation of a potential anti‐TB compound
Author(s) -
Sonopo Molahlehi S.,
Venter Kobus,
Winks Susan,
MarjanovicPainter Biljana,
Morgans Garreth L.,
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.3391
Subject(s) - chemistry , carbon 14 , distribution (mathematics) , tissue distribution , carbon fibers , medicine , physics , materials science , quantum mechanics , mathematical analysis , mathematics , composite number , composite material
This paper describes a five‐step synthesis of a carbon‐14‐labelled pyrazole compound (11). A total of 2.96 MBq of 11 was obtained with the specific activity of 2242.4 MBq/mmol. The radiochemical purity was >99%, and the overall radiochemical yield was 60% based on the [ 14 C 6 ] 4‐bromoaniline starting material. Biodistribution results showed that the radiotracer (administrated orally) has a high accumulation in the small intestine, large intestine and liver of both non‐infected and tuberculosis (TB)‐infected mice. Therefore, this suggests that compound 11 undergoes hepatobiliary clearance. The compound under investigation has been found to be slowly released from the liver between 2 and 8 h. The study revealed that 11 has no affinity for TB cells.