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

Therapeutic Approaches
Medicinal Chemistry

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.

Authors

Mott, Bryan T; Cheng, Ken Chih-Chien; Guha, Rajarshi; Kommer, Valerie P; Williams, David L; Vermeire, Jon J; Cappello, Michael; Maloney, David J; Rai Bantukallu, Ganesha; Jadhav, Ajit; Simeonov, Anton; Inglese, James; Posner, Gary H; Thomas, Craig;

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