A general method for tritium labelling of benzimidazole carbamates by catalytic exchange in dioxane solutions
✍ Scribed by Ernest Lacey; Michael Dawson; Mervyn A. Long; Chit Than
- Publisher
- John Wiley and Sons
- Year
- 1989
- Tongue
- French
- Weight
- 453 KB
- Volume
- 27
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Benzimidazole carbamates (BZCs) act as inhibitors of the tubulin-microtubule equilibria in eukaryotic organisms. Recently drug resistance to this class of compounds in helminth parasites has been shown to be due to a reduced ability of resistant tubulin to bind BZCs. In order to quantitate the nature of the tubulin-BZC interaction a general method for the specific tritium labelling of BZCs has been developed. The BZCs: mebendazole, oxfendazole, parbendazole, oxibendazole, albendazole and fenbendazole were labelled by catalytic exchange using palladium on calcium carbonate in pure dioxane at 60°C under tritium gas. The position of label incorporation for tritiated albendazole was determined by tritium-NMR as the 4-position of benzimidazole nucleus. The yields for individual BZCs varied from 8 to 68% for a range of specific activity of 0.44 to 13.4 Ci/mmole.