Carbon-14 radiolabelling and tissue distribution evaluation of a potential anti-TB compound
Date
2016Author
Sonopo, Molahlehi S.
Zeevaart, Jan R.
Venter, Kobus
Winks, Susan
Marjanovic-Painter, Biljana
Metadata
Show full item recordAbstract
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 [14C6] 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
URI
http://hdl.handle.net/10394/21226https://onlinelibrary.wiley.com/doi/abs/10.1002/jlcr.3391
https://doi.org/10.1002/jlcr.3391
Collections
- Faculty of Health Sciences [2404]