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ID: ALA3217651

Journal: Medchemcomm

Title: A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases().

Authors: Mott BT, Cheng KC, Guha R, Kommer VP, Williams DL, Vermeire JJ, Cappello M, Maloney DJ, Rai G, Jadhav A, Simeonov A, Inglese J, Posner GH, Thomas CJ.

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.

CiteXplore: 23205265

DOI: 10.1039/c2md20238g