| Autor: |
Papanastasiou, Ioannis, Tsotinis, Andrew, Foscolos, George B., Prathalingam, S. Radhika, Kelly, John M. |
| Zdroj: |
Journal of Heterocyclic Chemistry; September 2008, Vol. 45 Issue: 5 p1401-1406, 6p |
| Abstrakt: |
Aiming at the development of new adamantano building blocks for treating African trypanosomiasis, we report on the synthesis of spiro adamantane 2imidazolines 8afand 9ac, and their congeneric 51adamantylimidazolines 14and 15. The potency of these compounds against Trypanosoma bruceiwas compared to that of rimantadine and found, in the case of compound 14e, to be three fold higher. Together with the other active compounds, 14band 15b, which were equipotent to rimantadine, the new molecules illustrate the synergistic effect of the lipophilic character of adamantane and the C1 amidine functionality on trypanocidal activity. |
| Databáze: |
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