Carbon‐14 radiolabelling and tissue distribution evaluation of a potential anti‐TB compound |
| |
| Authors: | Molahlehi S. Sonopo Kobus Venter Susan Winks Biljana Marjanovic‐Painter Garreth L. Morgans Jan R. Zeevaart |
| |
| Affiliation: | 1. Radiochemistry, Necsa, Pretoria, South Africa;2. Medical Research Council of South Africa, Pretoria, South Africa;3. iThemba Pharmaceuticals (Pty) Ltd, Johannesburg, South Africa;4. DST/NWU, Preclinical Drug Development Platform, North West University, Potchefstroom, South Africa |
| |
| Abstract: | 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. |
| |
| Keywords: | pyrazole C‐14 labelling tuberculosis tissue distribution |
|
|
