Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites

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 a...

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Autores principales:	Szajnman, Sergio Hernán, Moreno, Silvia N. J., Rodríguez, Juan Bautista
Publicado:	2017
Materias:	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 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 Vero Cells
Acceso en línea:	https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_14203049_v22_n1_p_Galaka http://hdl.handle.net/20.500.12110/paper_14203049_v22_n1_p_Galaka
Aporte de:	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires

id	paper:paper_14203049_v22_n1_p_Galaka
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spelling	paper:paper_14203049_v22_n1_p_Galaka2023-06-08T16:13:34Z Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites Szajnman, Sergio Hernán Moreno, Silvia N. J. Rodríguez, Juan Bautista 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 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. Fil:Szajnman, S.H. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Moreno, S.N.J. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Rodriguez, J.B. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. 2017 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_14203049_v22_n1_p_Galaka http://hdl.handle.net/20.500.12110/paper_14203049_v22_n1_p_Galaka
institution	Universidad de Buenos Aires
institution_str	I-28
repository_str	R-134
collection	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA)
topic	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
spellingShingle	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 Szajnman, Sergio Hernán Moreno, Silvia N. J. Rodríguez, Juan Bautista Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites
topic_facet	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
description	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.
author	Szajnman, Sergio Hernán Moreno, Silvia N. J. Rodríguez, Juan Bautista
author_facet	Szajnman, Sergio Hernán Moreno, Silvia N. J. Rodríguez, Juan Bautista
author_sort	Szajnman, Sergio Hernán
title	Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites
title_short	Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites
title_full	Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites
title_fullStr	Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites
title_full_unstemmed	Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites
title_sort	antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites
publishDate	2017
url	https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_14203049_v22_n1_p_Galaka http://hdl.handle.net/20.500.12110/paper_14203049_v22_n1_p_Galaka
work_keys_str_mv	AT szajnmansergiohernan antiparasiticactivityofsulfurandfluorinecontainingbisphosphonatesagainsttrypanosomatidsandapicomplexanparasites AT morenosilvianj antiparasiticactivityofsulfurandfluorinecontainingbisphosphonatesagainsttrypanosomatidsandapicomplexanparasites AT rodriguezjuanbautista antiparasiticactivityofsulfurandfluorinecontainingbisphosphonatesagainsttrypanosomatidsandapicomplexanparasites
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Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites

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