| Literature DB >> 16942036 |
Steven J Burgess1, Audrey Selzer, Jane Xu Kelly, Martin J Smilkstein, Michael K Riscoe, David H Peyton.
Abstract
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[b,f]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.Entities:
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Year: 2006 PMID： 16942036 PMCID： PMC2215738 DOI： 10.1021/jm060399n
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446