A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseasesElectronic supplementary information (ESI) available. See DOI: 10.1039/c2md20238g

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...

Full description

Saved in:
Bibliographic Details
Main 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, Ganesha, Jadhav, Ajit, Simeonov, Anton, Inglese, James, Posner, Gary H, Thomas, Craig J
Format: Article
Language:English
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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 . A hybrid approach merged a 3-cyano-4-phenyl-1,2,5-oxadiazole 2-oxide (furoxan) with amodiaquine to create a potential therapeutic for malaria, schistosomiasis, and hookworm.
ISSN:2040-2503
2040-2511
DOI:10.1039/c2md20238g