2,4-Diarylthiazole antiprion compounds as a novel structural class of antimalarial leads


Thompson, MJ; Louth, JC; Little, SM; Chen, BN; Coldham, I; (2011) 2,4-Diarylthiazole antiprion compounds as a novel structural class of antimalarial leads. Bioorganic & medicinal chemistry letters, 21 (12). pp. 3644-3647. ISSN 0960-894X DOI: https://doi.org/10.1016/j.bmcl.2011.04.090

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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. (C) 2011 Elsevier Ltd. All rights reserved.

Item Type: Article
Keywords: Thiazoles, Amines, Dual activity, Malaria, Prion diseases, PRION DISEASE, QUINACRINE, DERIVATIVES, AGENTS
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Immunology and Infection
PubMed ID: 21570837
Web of Science ID: 291145900029
URI: http://researchonline.lshtm.ac.uk/id/eprint/533

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