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Quinoline Antimalarials Containing a Dibemethin Group are Active against Chloroquinone-Resistant Plasmodium falciparum and Inhibit Chloroquine Transport via the P. falciparum Chloroquine- Resistance Transporter (PfCRT)

Zishiri, Vincent K; Joshi, Mukesh C; Hunter, Roger; Chibale, Kelly; Smith, Peter J.; Summers, Robert; Martin, Rowena; Egan, Timothy J.


A series of 4-amino-7-chloroquinolines with dibenzylmethylamine (dibemethin) side chains were shown to inhibit synthetic hemozoin formation. These compounds were equally active against cultures of chloroquine-sensitive (D10) and chloroquine-resistant (K1) Plasmodium falciparum. The most active compound had an IC50 value comparable to that of chloroquine, and its potency was undiminished when tested in three additional chloroquine-resistant strains. The three most active compounds exhibited...[Show more]

CollectionsANU Research Publications
Date published: 2011
Type: Journal article
Source: Journal of Medicinal Chemistry
DOI: 10.1021/jm2009698


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