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Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: Further structure-activity relationships, in vivo studies, and preliminary toxicity profiling

Gemma, Sandra; Camodeca, Caterina; Coccone, Salvatore Sanna; Joshi, Bhupendra P; Bernetti, Matteo; Moretti, Vittoria; Brogi, Simone; de Marcos, Maria Cruz Bonache; Savini, Luisa; Taramelli, Donatella; Summers, Robert; Martin, Rowena


Despite recent progress in the fight against malaria, the emergence and spread of drug-resistant parasites remains a serious obstacle to the treatment of infections. We recently reported the development of a novel antimalarial drug that combines the 4-aminoquinoline pharmacophore of chloroquine with that of clotrimazole-based antimalarials. Here we describe the optimization of this class of hybrid drug through in-depth structure-activity relationship studies. Antiplasmodial properties and mode...[Show more]

CollectionsANU Research Publications
Date published: 2012
Type: Journal article
Source: Journal of Medicinal Chemistry
DOI: 10.1021/jm300802s


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