Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 18, Pages 6625-6633Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.08.001
Keywords
4-Aminoquinoline derivatives; Antimalarial agents; Chloroquine
Funding
- European Community [IP-018834]
- University of Milan [PUR 2008]
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A set of nine new arylpyrrolyl derivatives of 7-chloro-4-aminoquinoline, characterized by different substituents on the phenyl ring or different distance between the pyrrolic nitrogen and the 4-aminoquinoline, has been synthesized and tested for their activity against D-10 (CQ-S) and W-2 (CQ-R) strains of Plasmodium falciparum. All compounds exhibited activity against the CQ-S strain in the low nM range, comparable to that of chloroquine. Some of them were also highly active against the CQ-R strain and not toxic against normal cells. The antimalarial activity of this new class of compounds seems to be related to the inhibition of heme detoxification process of parasites, as in the case of chloroquine. (c) 2010 Elsevier Ltd. All rights reserved.
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