Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase

We have investigated the effect of a series of 1-amino-1,1-bisphosphonates derived from fatty acids against proliferation of the clinically more relevant form of Trypanosoma cruzi, the causative agent of American trypanosomiasis (Chagas' disease). Some of these drugs were potent inhibitors agai...

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Autores principales:	Szajnman, Sergio Hernán, Ravaschino, Esteban Luis, Rodríguez, Juan Bautista
Publicado:	2005
Materias:	Bisphosphonates Chagas' disease Farnesyl pyrophosphate synthase Trypanosoma cruzi bisphosphonic acid derivative fatty acid geranyltransferase protozoal protein antiprotozoal activity article cell proliferation Chagas disease drug synthesis drug targeting enzyme inhibition IC 50 nonhuman Animals Antiprotozoal Agents Diphosphonates Drug Delivery Systems Fatty Acids Inhibitory Concentration 50 Pyrophosphatases Structure-Activity Relationship
Acceso en línea:	https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v15_n21_p4685_Szajnman http://hdl.handle.net/20.500.12110/paper_0960894X_v15_n21_p4685_Szajnman
Aporte de:	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires

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spelling	paper:paper_0960894X_v15_n21_p4685_Szajnman2023-06-08T15:57:49Z Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase Szajnman, Sergio Hernán Ravaschino, Esteban Luis Rodríguez, Juan Bautista Bisphosphonates Chagas' disease Farnesyl pyrophosphate synthase Trypanosoma cruzi bisphosphonic acid derivative fatty acid geranyltransferase protozoal protein antiprotozoal activity article cell proliferation Chagas disease drug synthesis drug targeting enzyme inhibition IC 50 nonhuman Trypanosoma cruzi Animals Antiprotozoal Agents Diphosphonates Drug Delivery Systems Fatty Acids Inhibitory Concentration 50 Pyrophosphatases Structure-Activity Relationship Trypanosoma cruzi Trypanosoma cruzi We have investigated the effect of a series of 1-amino-1,1-bisphosphonates derived from fatty acids against proliferation of the clinically more relevant form of Trypanosoma cruzi, the causative agent of American trypanosomiasis (Chagas' disease). Some of these drugs were potent inhibitors against the intracellular form of the parasite, exhibiting IC50 values at low micromolar level. Cellular activity was associated with the inhibition of enzymatic activity of T. cruzi farnesyl pyrophosphate synthase. As bisphosphonate-containing drugs are FDA-approved for the treatment of bone resorption disorders, their potential innocuousness makes them good candidates to control tropical diseases. © 2005 Elsevier Ltd. All rights reserved. Fil:Szajnman, S.H. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Ravaschino, E.L. 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. 2005 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v15_n21_p4685_Szajnman http://hdl.handle.net/20.500.12110/paper_0960894X_v15_n21_p4685_Szajnman
institution	Universidad de Buenos Aires
institution_str	I-28
repository_str	R-134
collection	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA)
topic	Bisphosphonates Chagas' disease Farnesyl pyrophosphate synthase Trypanosoma cruzi bisphosphonic acid derivative fatty acid geranyltransferase protozoal protein antiprotozoal activity article cell proliferation Chagas disease drug synthesis drug targeting enzyme inhibition IC 50 nonhuman Trypanosoma cruzi Animals Antiprotozoal Agents Diphosphonates Drug Delivery Systems Fatty Acids Inhibitory Concentration 50 Pyrophosphatases Structure-Activity Relationship Trypanosoma cruzi Trypanosoma cruzi
spellingShingle	Bisphosphonates Chagas' disease Farnesyl pyrophosphate synthase Trypanosoma cruzi bisphosphonic acid derivative fatty acid geranyltransferase protozoal protein antiprotozoal activity article cell proliferation Chagas disease drug synthesis drug targeting enzyme inhibition IC 50 nonhuman Trypanosoma cruzi Animals Antiprotozoal Agents Diphosphonates Drug Delivery Systems Fatty Acids Inhibitory Concentration 50 Pyrophosphatases Structure-Activity Relationship Trypanosoma cruzi Trypanosoma cruzi Szajnman, Sergio Hernán Ravaschino, Esteban Luis Rodríguez, Juan Bautista Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase
topic_facet	Bisphosphonates Chagas' disease Farnesyl pyrophosphate synthase Trypanosoma cruzi bisphosphonic acid derivative fatty acid geranyltransferase protozoal protein antiprotozoal activity article cell proliferation Chagas disease drug synthesis drug targeting enzyme inhibition IC 50 nonhuman Trypanosoma cruzi Animals Antiprotozoal Agents Diphosphonates Drug Delivery Systems Fatty Acids Inhibitory Concentration 50 Pyrophosphatases Structure-Activity Relationship Trypanosoma cruzi Trypanosoma cruzi
description	We have investigated the effect of a series of 1-amino-1,1-bisphosphonates derived from fatty acids against proliferation of the clinically more relevant form of Trypanosoma cruzi, the causative agent of American trypanosomiasis (Chagas' disease). Some of these drugs were potent inhibitors against the intracellular form of the parasite, exhibiting IC50 values at low micromolar level. Cellular activity was associated with the inhibition of enzymatic activity of T. cruzi farnesyl pyrophosphate synthase. As bisphosphonate-containing drugs are FDA-approved for the treatment of bone resorption disorders, their potential innocuousness makes them good candidates to control tropical diseases. © 2005 Elsevier Ltd. All rights reserved.
author	Szajnman, Sergio Hernán Ravaschino, Esteban Luis Rodríguez, Juan Bautista
author_facet	Szajnman, Sergio Hernán Ravaschino, Esteban Luis Rodríguez, Juan Bautista
author_sort	Szajnman, Sergio Hernán
title	Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase
title_short	Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase
title_full	Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase
title_fullStr	Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase
title_full_unstemmed	Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase
title_sort	synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against trypanosoma cruzi targeting farnesyl pyrophosphate synthase
publishDate	2005
url	https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v15_n21_p4685_Szajnman http://hdl.handle.net/20.500.12110/paper_0960894X_v15_n21_p4685_Szajnman
work_keys_str_mv	AT szajnmansergiohernan synthesisandbiologicalevaluationof1amino11bisphosphonatesderivedfromfattyacidsagainsttrypanosomacruzitargetingfarnesylpyrophosphatesynthase AT ravaschinoestebanluis synthesisandbiologicalevaluationof1amino11bisphosphonatesderivedfromfattyacidsagainsttrypanosomacruzitargetingfarnesylpyrophosphatesynthase AT rodriguezjuanbautista synthesisandbiologicalevaluationof1amino11bisphosphonatesderivedfromfattyacidsagainsttrypanosomacruzitargetingfarnesylpyrophosphatesynthase
_version_	1768546310422528000

Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase

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