2,4-diarylthiazole antiprion compounds as a novel structural class of antimalarial leads |
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Authors: | Thompson Mark J Louth Jennifer C Little Susan M Chen Beining Coldham Iain |
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Institution: | a Department of Chemistry, University of Sheffield, Brook Hill, Sheffield S3 7HF, UK b Department of Immunology & Infection, Faculty of Infectious Tropical Diseases, London School of Hygiene & Tropical Medicine, Keppel Street, London WC1E 7HT, UK |
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Abstract: | A significant intersection between antimalarial and antiprion activity is well established for certain compound classes, specifically for polycyclic antimalarial agents bearing basic nitrogen-containing sidechains (e.g., chloroquine, quinacrine, mefloquine). Screening a recently reported set of antiprion compounds with such sidechains showed these 2,4-diarylthiazole based structures also possess significant antimalarial activity. Of particular note, all but one of the compounds displayed activity against a chloroquine-resistant Plasmodium falciparum strain, identifying them as interesting leads for further development in this context. In addition, three new members of the series showed superior antiprion activity compared to the earlier-reported compounds. |
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Keywords: | Thiazoles Amines Dual activity Malaria Prion diseases |
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