Artículo

Galaka, T.; Casal, M.F.; Storey, M.; Li, C.; Chao, M.N.; Szajnman, S.H.; Docampo, R.; Moreno, S.N.J.; Rodriguez, J.B."Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites" (2017) Molecules. 22(1)
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Abstract:

Based on crystallographic data of the complexes 2-alkyl(amino)ethyl-1,1-bisphosphonates-Trypanosoma cruzi farnesyl diphosphate synthase, some linear 1,1-bisphosphonic acids and other closely related derivatives were designed, synthesized and biologically evaluated against T. cruzi, the responsible agent of Chagas disease and against Toxoplasma gondii, the etiologic agent of toxoplasmosis and also towards the target enzymes farnesyl pyrophosphate synthase of T. cruzi (TcFPPS) and T gondii (TgFPPS), respectively. The isoprenoid-containing 1,1-bisphosphonates exhibited modest antiparasitic activity, whereas the linear α-fluoro-2-alkyl(amino)ethyl-1,1-bisphosphonates were unexpectedly devoid of antiparasitic activity. In spite of not presenting efficient antiparasitic activity, these data turned out to be very important to establish a structural activity relationship. © 2017 by the authors; licensee MDPI, Basel, Switzerland.

Registro:

Documento: Artículo
Título:Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites
Autor:Galaka, T.; Casal, M.F.; Storey, M.; Li, C.; Chao, M.N.; Szajnman, S.H.; Docampo, R.; Moreno, S.N.J.; Rodriguez, J.B.
Filiación:Departamento de Química Orgánica and UMYMFOR (CONICET-FCEyN), Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Pabellón 2, Buenos Aires, C1428EHA, Argentina
Center for Tropical and Emerging Global Diseases, Department of Cellular Biology, University of Georgia, Athens, GA 30602, United States
Palabras clave:Antiparasitic agents; Bisphosphonates; Chagas disease; Farnesyl diphosphate synthase; Toxoplasma gondii; Toxoplasmosis; Trypanosoma cruzi; antiprotozoal agent; bisphosphonic acid derivative; enzyme inhibitor; geranyltransferase; protozoal protein; animal; antagonists and inhibitors; Chlorocebus aethiops; drug effects; drug sensitivity; enzyme assay; enzymology; gene expression; genetics; growth, development and aging; halogenation; human; metabolism; structure activity relation; synthesis; Toxoplasma; Trypanosoma cruzi; Vero cell line; Animals; Antiprotozoal Agents; Cercopithecus aethiops; Diphosphonates; Enzyme Assays; Enzyme Inhibitors; Gene Expression; Geranyltranstransferase; Halogenation; Humans; Parasitic Sensitivity Tests; Protozoan Proteins; Structure-Activity Relationship; Toxoplasma; Trypanosoma cruzi; Vero Cells
Año:2017
Volumen:22
Número:1
DOI: http://dx.doi.org/10.3390/molecules22010082
Handle:http://hdl.handle.net/20.500.12110/paper_14203049_v22_n1_p_Galaka
Título revista:Molecules
Título revista abreviado:Molecules
ISSN:14203049
CODEN:MOLEF
CAS:geranyltransferase, 37277-79-5, 50812-36-7; Antiprotozoal Agents; Diphosphonates; Enzyme Inhibitors; Geranyltranstransferase; Protozoan Proteins
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_14203049_v22_n1_p_Galaka

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Citas:

---------- APA ----------
Galaka, T., Casal, M.F., Storey, M., Li, C., Chao, M.N., Szajnman, S.H., Docampo, R.,..., Rodriguez, J.B. (2017) . Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites. Molecules, 22(1).
http://dx.doi.org/10.3390/molecules22010082
---------- CHICAGO ----------
Galaka, T., Casal, M.F., Storey, M., Li, C., Chao, M.N., Szajnman, S.H., et al. "Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites" . Molecules 22, no. 1 (2017).
http://dx.doi.org/10.3390/molecules22010082
---------- MLA ----------
Galaka, T., Casal, M.F., Storey, M., Li, C., Chao, M.N., Szajnman, S.H., et al. "Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites" . Molecules, vol. 22, no. 1, 2017.
http://dx.doi.org/10.3390/molecules22010082
---------- VANCOUVER ----------
Galaka, T., Casal, M.F., Storey, M., Li, C., Chao, M.N., Szajnman, S.H., et al. Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites. Molecules. 2017;22(1).
http://dx.doi.org/10.3390/molecules22010082