Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 22, Issue 21, Pages 5950-5960Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.09.009
Keywords
4-Aminoquinolines; Chiral chloroquine analogues; Chloroquine resistant stain
Funding
- CSIR, New Delhi
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In this investigation, we describe a new approach to chiral synthesis of chloroquine and its analogues. All tested compounds displayed potent activity against chloroquine sensitive as well as chloroquine resistant strains of Plasmodium falciparum in vitro and Plasmodium yoelii in vivo. Compounds S-13b, S-13c, S-13d and S-13i displayed excellent in vitro antimalarial activity with an IC50 value of 56.82, 60.41, 21.82 and 7.94 nM, respectively, in the case of resistant strain. Furthermore, compounds S-13a, S-13c and S-13d showed in vivo suppression of 100% parasitaemia on day 4 in the mouse model against Plasmodium yoelii when administered orally. These results underscore the application of synthetic methodology and need for further lead optimization. (C) 2014 Elsevier Ltd. All rights reserved.
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