Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 18, Pages 5623-5625Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm060399n
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Funding
- NIAID NIH HHS [R21 AI067837-01A2, R21 AI067837] Funding Source: Medline
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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-methylpropane1,3- 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.
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