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

…, R Hunter, PJ Smith, D Taylor, R Summers…

Index: Zishiri, Vincent K.; Hunter, Roger; Smith, Peter J.; Taylor, Dale; Summers, Robert; Kirk, Kiaran; Martin, Rowena E.; Egan, Timothy J. European Journal of Medicinal Chemistry, 2011 , vol. 46, # 5 p. 1729 - 1742

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Citation Number: 13

Abstract

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, ...