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

doi:10.1021/jm300802s

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Article

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

Journal of medicinal chemistry - 9 Aug 2012

Gemma Sandra, Camodeca Caterina, Sanna Coccone Salvatore, Joshi Bhupendra P, Bernetti Matteo, Moretti Vittoria, Brogi Simone, Bonache de Marcos Maria Cruz, Savini Luisa, Taramelli Donatella, Basilico Nicoletta, Parapini Silvia, Rottmann Matthias, Brun Reto, Lamponi Stefania, Caccia Silvio, Guiso Giovanna, Summers Robert L, Martin Rowena E, Saponara Simona, Gorelli Beatrice, Novellino Ettore, Campiani Giuseppe, Butini Stefania

Abstract excerpt

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...

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PMID: 22783984
DOI: 10.1021/jm300802s

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

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