Synthesis, Antiplasmodial Activity, and β-Hematin Inhibition of Hydroxypyridone–Chloroquine Hybrids

…, TJ Egan, J Gut, PJ Rosenthal, K Chibale

Index: Andayi, Warren A.; Egan, Timothy J.; Gut, Jiri; Rosenthal, Philip J.; Chibale, Kelly ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 7 p. 642 - 646

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Citation Number: 15

Abstract

A series of noncytotoxic 4-aminoquinoline-3-hydroxypyridin-4-one hybrids were synthesized on the basis of a synergistic in vitro combination of a precursor N-alkyl-3-hydroxypyridin-4- one with chloroquine (CQ) and tested in vitro against CQ resistant (K1 and W2) and sensitive (3D7) strains of Plasmodium falciparum. In vitro antiplasmodial activity of the precursors was negated by blocking the chelator moiety via complexation with gallium (III) ...