title: A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases().
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.affiliation: Department of Chemistry, Zanvyl Krieger School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, Maryland, 21218, USA ; Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland, 20892, USA.
authors.forename: Bryan T
authors.initials: BT
authors.lastname: Mott
authors.forename: Ken Chih-Chien
authors.initials: KC
authors.lastname: Cheng
authors.forename: Rajarshi
authors.initials: R
authors.lastname: Guha
authors.forename: Valerie P
authors.initials: VP
authors.lastname: Kommer
authors.forename: David L
authors.initials: DL
authors.lastname: Williams
authors.forename: Jon J
authors.initials: JJ
authors.lastname: Vermeire
authors.forename: Michael
authors.initials: M
authors.lastname: Cappello
authors.forename: David J
authors.initials: DJ
authors.lastname: Maloney
authors.forename: Ganesha
authors.initials: G
authors.lastname: Rai
authors.forename: Ajit
authors.initials: A
authors.lastname: Jadhav
authors.forename: Anton
authors.initials: A
authors.lastname: Simeonov
authors.forename: James
authors.initials: J
authors.lastname: Inglese
authors.forename: Gary H
authors.initials: GH
authors.lastname: Posner
authors.forename: Craig J
authors.initials: CJ
authors.lastname: Thomas