Design, Synthesis, and Evaluation of Novel Ferroquine and Phenylequine Analogues as Potential Antiplasmodial Agents.

Authors :: Jacobs L
de Kock C
de Villiers KA
Smith PJ
Smith VJ
van Otterlo WA
Blackie MA
Source :: ChemMedChem [ChemMedChem] 2015 Dec; Vol. 10 (12), pp. 2099-110. Date of Electronic Publication: 2015 Oct 08.
Publication Year :: 2015
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.<br /> (© 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

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