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Parallel synthesis and anti-malarial activity of a sulfonamide library |
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| Authors: | Ryckebusch A Déprez-Poulain R Debreu-Fontaine M A Vandaele R Mouray E Grellier P Sergheraert C |
| Affiliation: | Institut de Biologie et Institut Pasteur de Lille, UMR CNRS 8525, Université de Lille II, 1 rue du Professeur Calmette, B.P. 447, 59021, Lille, France. |
| Abstract: | Solution-phase synthesis and evaluation of a library of 31 sulfonamides as inhibitors of a chloroquine-resistant strain of Plasmodium falciparum are described. The most potent compound displayed an activity 100-fold better than chloroquine. Experiments using a fluorescent sulfonamide derivative suggest that their site of action inside the parasite is different to that of chloroquine. |
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