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Preparation of a pyrimethamine lipophile by chemical modification : a comparative study of the action of pyrimethamine and N-2-oleyl pyrimethaminamide derivative on Toxoplasma gondii |
Oléagineux, Corps Gras, Lipides. Volume 6, Number 3, 260-6, Mai - Juin 1999, Fondamental
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 Résumé
 Summary
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Author(s) : Zéphirin MOULOUNGUI, Bahipi KIMPIOBI-NINAFIDING, Gilles FAVRE, Nicole DUMAS. |
Summary : The acylation of pyrimethamine by oleic acid was brought about by trifluoroacetic anhydride in the presence of cation exchange resins, anion exchange resins and adsorbent resins. The reaction occurred within 4 hours at moderate temperature (65°C) in a biphasic solid-liquid system. These solid polymer supports gave 60% to 80% yields of N-2-oleyl pyrimethaminamide from monoacylation of the pyrimethamine. The action of the derivative was compared with that of pyrimethamine on Toxoplasma gondii grown on fibroblasts in culture and in mice. The N-2-oleyl pyrimethaminamide was highly active against Toxoplasma gondii in cell cultures, but showed no effect on the intracellular multiplication of Toxoplasma gondii, in cytological studies. |
Keywords : pyrimethamine, lipophilic pyrimethaminamide, ion exchange resins, N-acylation, Toxoplasma gondii, fibroblasts. |
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