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Issue 12, 2012
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A furoxan–amodiaquine hybrid as a potential therapeutic for three parasitic diseases

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Abstract

Parasitic diseases continue to have a devastating impact on human populations worldwide. Lack of effective treatments, the high cost of existing ones, and frequent emergence of resistance to these agents provide a strong argument for the development of novel therapies. Here we report the results of a hybrid approach designed to obtain a dual acting molecule that would demonstrate activity against a variety of parasitic targets. The antimalarial drug amodiaquine has been covalently joined with a nitric oxide-releasing furoxan to achieve multiple mechanisms of action. Using in vitro and ex vivo assays, the hybrid molecule shows activity against three parasites – Plasmodium falciparum, Schistosoma mansoni, and Ancylostoma ceylanicum.

Graphical abstract: A furoxan–amodiaquine hybrid as a potential therapeutic for three parasitic diseases

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Supplementary files

Article information


Submitted
09 Aug 2012
Accepted
27 Sep 2012
First published
03 Oct 2012

Med. Chem. Commun., 2012,3, 1505-1511
Article type
Concise Article

A furoxanamodiaquine hybrid as a potential therapeutic for three parasitic diseases

B. T. Mott, K. C. Cheng, R. Guha, V. P. Kommer, D. L. Williams, J. J. Vermeire, M. Cappello, D. J. Maloney, G. Rai, A. Jadhav, A. Simeonov, J. Inglese, G. H. Posner and C. J. Thomas, Med. Chem. Commun., 2012, 3, 1505
DOI: 10.1039/C2MD20238G

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