Design,Synthesis, and Evaluation of Novel Ferroquine and Phenylequine Analogues as Potential Antiplasmodial Agents |
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| Authors: | Leon Jacobs Dr Carmen de Kock Dr Katherine A de Villiers Prof Peter J Smith Dr Vincent J Smith Prof Willem A L van Otterlo Dr Margaret A L Blackie |
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| Affiliation: | 1. Department of Chemistry and Polymer Science, Stellenbosch University, Matieland, South Africa;2. Department of Pharmacology, University of Cape Town, Cape Town, South Africa |
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| Abstract: | 7‐Chloroquinoline‐based antimalarial drugs are effective in the inhibition of hemozoin formation in the food vacuole of the Plasmodium parasite, the causative agent of malaria. We synthesized five series of ferroquine (FQ) and phenylequine (PQ) derivatives, which display good in vitro efficacy toward both the chloroquine‐sensitive (CQS) NF54 (IC50: 4.2 nm ) and chloroquine‐resistant (CQR) Dd2 (IC50: 33.7 nm ) strains of P. falciparum. Several compounds were found to have good inhibitory activity against β‐hematin formation in an NP‐40 detergent assay, with IC50 values ranging between 10.4 and 19.2 μm . |
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| Keywords: | β -hematin ferroquine malaria oxalamide phenylequine |
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