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Issue 12, 2012
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A furoxanamodiaquine 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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Publication details

The article was received on 09 Aug 2012, accepted on 27 Sep 2012 and first published on 03 Oct 2012


Article type: Concise Article
DOI: 10.1039/C2MD20238G
Citation: Med. Chem. Commun., 2012,3, 1505-1511
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    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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