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A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases().
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.
Afiliação
  • Mott BT; 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.
Medchemcomm ; 3(12): 1505-1511, 2012 Dec.
Article em En | MEDLINE | ID: mdl-23205265
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.

Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2012 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2012 Tipo de documento: Article