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: Galaka, Tamila Pavlivna, Ferrer, Mariana, Storey, Melissa, Li, Catherine, Chao, Maria Noelia, Szajnman, Sergio Hernan, Docampo, Roberto, Moreno, Silvia N. J., Rodriguez, Juan Bautista
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2017
País:Argentina
Institución:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/60217
Acceso en línea:http://hdl.handle.net/11336/60217
Access Level:acceso abierto
Palabra clave:ANTIPARASITIC AGENTS
BISPHOSPHONATES
CHAGAS DISEASE
FARNESYL DIPHOSPHATE SYNTHASE
TOXOPLASMA GONDII
TOXOPLASMOSIS
TRYPANOSOMA CRUZI
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
id AR_16c2fcb320bbee9ff336b620cc34fe20
oai_identifier_str oai:ri.conicet.gov.ar:11336/60217
network_acronym_str AR
network_name_str Argentina
repository_id_str
dc.title.none.fl_str_mv Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites
title Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites
spellingShingle Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites
Galaka, Tamila Pavlivna
ANTIPARASITIC AGENTS
BISPHOSPHONATES
CHAGAS DISEASE
FARNESYL DIPHOSPHATE SYNTHASE
TOXOPLASMA GONDII
TOXOPLASMOSIS
TRYPANOSOMA CRUZI
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
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
dc.creator.none.fl_str_mv Galaka, Tamila Pavlivna
Ferrer, Mariana
Storey, Melissa
Li, Catherine
Chao, Maria Noelia
Szajnman, Sergio Hernan
Docampo, Roberto
Moreno, Silvia N. J.
Rodriguez, Juan Bautista
author Galaka, Tamila Pavlivna
author_facet Galaka, Tamila Pavlivna
Ferrer, Mariana
Storey, Melissa
Li, Catherine
Chao, Maria Noelia
Szajnman, Sergio Hernan
Docampo, Roberto
Moreno, Silvia N. J.
Rodriguez, Juan Bautista
author_role author
author2 Ferrer, Mariana
Storey, Melissa
Li, Catherine
Chao, Maria Noelia
Szajnman, Sergio Hernan
Docampo, Roberto
Moreno, Silvia N. J.
Rodriguez, Juan Bautista
author2_role author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv ANTIPARASITIC AGENTS
BISPHOSPHONATES
CHAGAS DISEASE
FARNESYL DIPHOSPHATE SYNTHASE
TOXOPLASMA GONDII
TOXOPLASMOSIS
TRYPANOSOMA CRUZI
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
topic ANTIPARASITIC AGENTS
BISPHOSPHONATES
CHAGAS DISEASE
FARNESYL DIPHOSPHATE SYNTHASE
TOXOPLASMA GONDII
TOXOPLASMOSIS
TRYPANOSOMA CRUZI
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
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.
publishDate 2017
dc.date.none.fl_str_mv 2017-01
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/60217
Galaka, Tamila Pavlivna; Ferrer, Mariana; Storey, Melissa; Li, Catherine; Chao, Maria Noelia; et al.; Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites; Molecular Diversity Preservation International; Molecules; 22; 1; 1-2017; 1-22
1420-3049
CONICET Digital
CONICET
url http://hdl.handle.net/11336/60217
identifier_str_mv Galaka, Tamila Pavlivna; Ferrer, Mariana; Storey, Melissa; Li, Catherine; Chao, Maria Noelia; et al.; Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites; Molecular Diversity Preservation International; Molecules; 22; 1; 1-2017; 1-22
1420-3049
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.3390/molecules22010082
info:eu-repo/semantics/altIdentifier/url/http://www.mdpi.com/1420-3049/22/1/82
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
application/pdf
application/pdf
application/pdf
dc.publisher.none.fl_str_mv Molecular Diversity Preservation International
publisher.none.fl_str_mv Molecular Diversity Preservation International
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
_version_ 1799195700667351040
spelling Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasitesGalaka, Tamila PavlivnaFerrer, MarianaStorey, MelissaLi, CatherineChao, Maria NoeliaSzajnman, Sergio HernanDocampo, RobertoMoreno, Silvia N. J.Rodriguez, Juan BautistaANTIPARASITIC AGENTSBISPHOSPHONATESCHAGAS DISEASEFARNESYL DIPHOSPHATE SYNTHASETOXOPLASMA GONDIITOXOPLASMOSISTRYPANOSOMA CRUZIhttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1Based 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.Fil: Galaka, Tamila Pavlivna. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos en Química Orgánica. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Unidad de Microanálisis y Métodos Físicos en Química Orgánica; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Química Orgánica; ArgentinaFil: Ferrer, Mariana. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos en Química Orgánica. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Unidad de Microanálisis y Métodos Físicos en Química Orgánica; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Química Orgánica; ArgentinaFil: Storey, Melissa. University of Georgia; Estados UnidosFil: Li, Catherine. University of Georgia; Estados UnidosFil: Chao, Maria Noelia. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos en Química Orgánica. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Unidad de Microanálisis y Métodos Físicos en Química Orgánica; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Química Orgánica; ArgentinaFil: Szajnman, Sergio Hernan. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos en Química Orgánica. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Unidad de Microanálisis y Métodos Físicos en Química Orgánica; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Química Orgánica; ArgentinaFil: Docampo, Roberto. University of Georgia; Estados UnidosFil: Moreno, Silvia N. J.. University of Georgia; Estados UnidosFil: Rodriguez, Juan Bautista. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Unidad de Microanálisis y Métodos Físicos en Química Orgánica. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Unidad de Microanálisis y Métodos Físicos en Química Orgánica; Argentina. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Departamento de Química Orgánica; ArgentinaMolecular Diversity Preservation International2017-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/60217Galaka, Tamila Pavlivna; Ferrer, Mariana; Storey, Melissa; Li, Catherine; Chao, Maria Noelia; et al.; Antiparasitic activity of sulfur- and fluorine-containing bisphosphonates against trypanosomatids and apicomplexan parasites; Molecular Diversity Preservation International; Molecules; 22; 1; 1-2017; 1-221420-3049CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.3390/molecules22010082info:eu-repo/semantics/altIdentifier/url/http://www.mdpi.com/1420-3049/22/1/82info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2024-05-08T14:00:47Zoai:ri.conicet.gov.ar:11336/60217instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982024-05-08 14:00:48.068CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
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