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Artículo

Fluorine-containing aryloxyethyl thiocyanate derivatives are potent inhibitors of Trypanosoma cruzi and Toxoplasma gondii proliferation

Garcia Liñares, Guadalupe EugeniaIcon ; Gismondi, Santiago; Osa Codesido, NicolasIcon ; Moreno, Silvia N. J.; Docampo, Roberto; Rodriguez, Juan BautistaIcon
Fecha de publicación: 09/2007
Editorial: Pergamon-Elsevier Science Ltd
Revista: Biorganic and Medicinal Chemistry Letters
ISSN: 0960-894X
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:
Otras Ciencias Químicas

Resumen

As a part of our project aimed at developing new safe chemotherapeutic and chemoprophylactic agents against tropical diseases, fluorine-containing drugs structurally related to 4-phenoxyphenoxyethyl thiocyanate (1) were designed, synthesized, and evaluated as antiproliferative agents against Trypanosoma cruzi, the parasite responsible of American trypanosomiasis (Chagas' disease), and Toxoplasma gondii, the etiological agent of toxoplasmosis. This thiocyanate derivative had previously proven to be an effective agent against T. cruzi proliferation. Fluorine-containing thiocyanate derivatives 2 and 3 were threefold more potent than our lead drug 1 against intracellular T. cruzi. The biological evaluation against T. gondii was also very promising. The IC50 values corresponding to 2 and 3 were at the very low micromolar level against tachyzoites of T. gondii. Both of these drugs are interesting examples of effective antiparasitic agents that have outstanding potential not only as lead drugs but also to be used for further in vivo studies.
Palabras clave: Aryloxyethyl Thiocyanates , Chagas' Disease , Squalene Synthase , Toxoplasma Gondii , Trypanosoma Cruzi
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info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Atribución-NoComercial-SinDerivadas 2.5 Argentina (CC BY-NC-ND 2.5 AR)
Identificadores
URI: http://hdl.handle.net/11336/70787
DOI: http://dx.doi.org/10.1016/j.bmcl.2007.07.012
URL: https://www.sciencedirect.com/science/article/pii/S0960894X07008141
URL: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4078023/
Colecciones
Articulos(UMYMFOR)
Articulos de UNID.MICROANAL.Y MET.FISICOS EN QUIM.ORG.(I)
Citación
Garcia Liñares, Guadalupe Eugenia; Gismondi, Santiago; Osa Codesido, Nicolas; Moreno, Silvia N. J.; Docampo, Roberto; et al.; Fluorine-containing aryloxyethyl thiocyanate derivatives are potent inhibitors of Trypanosoma cruzi and Toxoplasma gondii proliferation; Pergamon-Elsevier Science Ltd; Biorganic and Medicinal Chemistry Letters; 17; 18; 9-2007; 5068-5071
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