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A series of structurally simple chloroquine chemosensitizing dibemethin derivatives that inhibit chloroquine transport by PfCRT

Zishiri, Vincent K; Hunter, Roger; Smith, Peter J.; Taylor, Dale; Summers, Robert; Kirk, Kiaran; Martin, Rowena; Egan, Timothy J.


A series of 12 new dibemethin (N-benzyl-N-methyl-1-phenylmethanamine) derivatives bearing an N-aminomethyl group attached to the one phenyl ring and an H, Cl, OCH3 or N(CH3)2 group on the other have been synthesized. These compounds all showed strong chloroquine chemosensitizing activity, comparable to verapamil, when present at 1 μM in an in vitro culture of the chloroquine-resistant W2 strain of the human malaria parasite, Plasmodium falciparum. Their N-formylated derivatives also exhibited...[Show more]

CollectionsANU Research Publications
Date published: 2011
Type: Journal article
Source: European Journal of Medicinal Chemistry
DOI: 10.1016/j.ejmech.2011.02.026


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