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Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds

Burgess, S. J. and Kelly, J. X. and Shomloo, S. and Wittlin, S. and Brun, R. and Liebmann, K. and Peyton, D. H.. (2010) Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. Journal of medicinal chemistry, 53 (17). pp. 6477-6489.

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Official URL: http://edoc.unibas.ch/dok/A5843035

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Abstract

We have previously shown that a 'reversed chloroquine (RCQ)' molecule, composed of a chloroquine-like moiety and a resistance reversal-like moiety, can overcome chloroquine resistance in P. falciparum ( Burgess , S. J. ; Selzer , A. ; Kelly , J. X. ; Smilkstein , M. J. ; Riscoe , M. K. ; Peyton , D. H. J. Med. Chem. 2006 , 49 , 5623 . Andrews , S. ; Burgess , S. J. ; Skaalrud , D. ; Kelly , J. X. ; Peyton , D. H. J. Med. Chem. 2010 , 53 , 916 ). Here, we present an investigation into the structure-activity relationship of the RCQ structures, resulting in an orally active molecule with good in vitro and in vivo antimalarial activity. We also present evidence of the mode of action, indicating that the RCQ molecules inhibit hemozoin formation in the parasite's digestive vacuole in a manner similar to that of chloroquine
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Brun, Reto and Wittlin, Sergio
Item Type:Article, refereed
Bibsysno:Link to catalogue
Publisher:American Chemical Society
ISSN:0022-2623
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:19 Oct 2017 07:13
Deposited On:14 Sep 2012 06:46

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