title: 2,4-diarylthiazole antiprion compounds as a novel structural class of antimalarial leads.
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.
authors.affiliation: Department of Chemistry, University of Sheffield, Brook Hill, Sheffield, UK. m.j.thompson@sheffield.ac.uk
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Thompson
authors.forename: Jennifer C
authors.initials: JC
authors.lastname: Louth
authors.forename: Susan M
authors.initials: SM
authors.lastname: Little
authors.forename: Beining
authors.initials: B
authors.lastname: Chen
authors.forename: Iain
authors.initials: I
authors.lastname: Coldham
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002738:Chloroquine / Q000737:chemistry / Q000494:pharmacology; D015767:Mefloquine / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects*; D011328:Prions / Q000037:antagonists & inhibitors*; D011796:Quinacrine / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000962:Antimalarials; D011328:Prions; D013844:Thiazoles; D002738:Chloroquine; D011796:Quinacrine; D015767:Mefloquine