A chloroquine-like molecule designed to reverse resistance in Plasmodium falciparum

Steven J. Burgess, Audrey Selzer, Jane Xu Kelly, Martin J. Smilkstein, Michael K. Riscoe, David H. Peyton

Research output: Contribution to journalArticlepeer-review

124 Scopus citations


A class of hybrid molecules which we term 'reversed chloroquines' (RCQs) was designed, and a prototype molecule, N′-(7-chloroquinolin-4-yl)-N-[3- (10,11-dihydrodibenzo[bf]azepin-5-yl)propyl]-N-methylpropane-1,3-diamine (1), was synthesized and tested against both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. An in vitro assay against the two strains indicated that 1 was effective at low-nM concentrations against both strains. A preliminary study in mice demonstrated oral efficacy against P. chabaudi and the absence of obvious toxicity. The RCQ approach therefore appears to be feasible.

Original languageEnglish (US)
Pages (from-to)5623-5625
Number of pages3
JournalJournal of Medicinal Chemistry
Issue number18
StatePublished - Sep 7 2006
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


Dive into the research topics of 'A chloroquine-like molecule designed to reverse resistance in Plasmodium falciparum'. Together they form a unique fingerprint.

Cite this