Synthesis and antikinetoplastid activity of a series of N,N′-substituted diamines

Autores
Caminos, Andrea P.; Panozzo Zenere, Esteban Andrés; Wilkinson, Shane. R.; Tekwani, Babu L.; Labadie, Guillermo Roberto
Año de publicación
2012
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
A series of 25 N,N-substituted diamines were prepared by controlled reductive amination of free aliphatic diamines with different substituted benzaldehydes. The library was screened in vitro for antiparasitic activity on the causative agents of human African trypanosomiasis, Chagas’ disease and visceral leishmaniasis. The most potent compounds were derived from a subset of diamines that contained a 4-OBn substitution, having a 50% parasite growth inhibition in the submicromolar (against Trypanosoma cruzi) or nanomolar (against Trypanosoma brucei and Leishmania donovani) range. We conclude that members of this series of N,N´-substituted diamines provide new lead structures that have potential to treat trypanosomal and leishmanial infections.
Fil: Caminos, Andrea P.. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
Fil: Panozzo Zenere, Esteban Andrés. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
Fil: Wilkinson, Shane. R.. University of London; Reino Unido
Fil: Tekwani, Babu L.. University of Mississippi; Estados Unidos
Fil: Labadie, Guillermo Roberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
Materia
LEISHMANIASIS
CHAGAS DIEASE
HUMAN AFRICAN TRYPANOSOMIASIS
DIAMINES
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/111686
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/111686
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Synthesis and antikinetoplastid activity of a series of N,N′-substituted diaminesCaminos, Andrea P.Panozzo Zenere, Esteban AndrésWilkinson, Shane. R.Tekwani, Babu L.Labadie, Guillermo RobertoLEISHMANIASISCHAGAS DIEASEHUMAN AFRICAN TRYPANOSOMIASISDIAMINEShttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1A series of 25 N,N-substituted diamines were prepared by controlled reductive amination of free aliphatic diamines with different substituted benzaldehydes. The library was screened in vitro for antiparasitic activity on the causative agents of human African trypanosomiasis, Chagas’ disease and visceral leishmaniasis. The most potent compounds were derived from a subset of diamines that contained a 4-OBn substitution, having a 50% parasite growth inhibition in the submicromolar (against Trypanosoma cruzi) or nanomolar (against Trypanosoma brucei and Leishmania donovani) range. We conclude that members of this series of N,N´-substituted diamines provide new lead structures that have potential to treat trypanosomal and leishmanial infections.Fil: Caminos, Andrea P.. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; ArgentinaFil: Panozzo Zenere, Esteban Andrés. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; ArgentinaFil: Wilkinson, Shane. R.. University of London; Reino UnidoFil: Tekwani, Babu L.. University of Mississippi; Estados UnidosFil: Labadie, Guillermo Roberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; ArgentinaPergamon-Elsevier Science Ltd2012-02-15info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/111686Caminos, Andrea P.; Panozzo Zenere, Esteban Andrés; Wilkinson, Shane. R.; Tekwani, Babu L.; Labadie, Guillermo Roberto; Synthesis and antikinetoplastid activity of a series of N,N′-substituted diamines; Pergamon-Elsevier Science Ltd; Bioorganic & Medicinal Chemistry Letters; 22; 4; 15-2-2012; 1712-17150960-894XCONICET DigitalCONICETengCorregido en https://doi.org/10.1016/j.bmcl.2013.02.003info:eu-repo/semantics/altIdentifier/doi/10.1016/j.bmcl.2011.12.101info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/abs/pii/S0960894X11017835info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-10T13:09:24Zoai:ri.conicet.gov.ar:11336/111686instacron: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:34982025-09-10 13:09:24.896CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Synthesis and antikinetoplastid activity of a series of N,N′-substituted diamines
title Synthesis and antikinetoplastid activity of a series of N,N′-substituted diamines
spellingShingle Synthesis and antikinetoplastid activity of a series of N,N′-substituted diamines
Caminos, Andrea P.
LEISHMANIASIS
CHAGAS DIEASE
HUMAN AFRICAN TRYPANOSOMIASIS
DIAMINES
title_short Synthesis and antikinetoplastid activity of a series of N,N′-substituted diamines
title_full Synthesis and antikinetoplastid activity of a series of N,N′-substituted diamines
title_fullStr Synthesis and antikinetoplastid activity of a series of N,N′-substituted diamines
title_full_unstemmed Synthesis and antikinetoplastid activity of a series of N,N′-substituted diamines
title_sort Synthesis and antikinetoplastid activity of a series of N,N′-substituted diamines
dc.creator.none.fl_str_mv Caminos, Andrea P.
Panozzo Zenere, Esteban Andrés
Wilkinson, Shane. R.
Tekwani, Babu L.
Labadie, Guillermo Roberto
author Caminos, Andrea P.
author_facet Caminos, Andrea P.
Panozzo Zenere, Esteban Andrés
Wilkinson, Shane. R.
Tekwani, Babu L.
Labadie, Guillermo Roberto
author_role author
author2 Panozzo Zenere, Esteban Andrés
Wilkinson, Shane. R.
Tekwani, Babu L.
Labadie, Guillermo Roberto
author2_role author
author
author
author
dc.subject.none.fl_str_mv LEISHMANIASIS
CHAGAS DIEASE
HUMAN AFRICAN TRYPANOSOMIASIS
DIAMINES
topic LEISHMANIASIS
CHAGAS DIEASE
HUMAN AFRICAN TRYPANOSOMIASIS
DIAMINES
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv A series of 25 N,N-substituted diamines were prepared by controlled reductive amination of free aliphatic diamines with different substituted benzaldehydes. The library was screened in vitro for antiparasitic activity on the causative agents of human African trypanosomiasis, Chagas’ disease and visceral leishmaniasis. The most potent compounds were derived from a subset of diamines that contained a 4-OBn substitution, having a 50% parasite growth inhibition in the submicromolar (against Trypanosoma cruzi) or nanomolar (against Trypanosoma brucei and Leishmania donovani) range. We conclude that members of this series of N,N´-substituted diamines provide new lead structures that have potential to treat trypanosomal and leishmanial infections.
Fil: Caminos, Andrea P.. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
Fil: Panozzo Zenere, Esteban Andrés. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
Fil: Wilkinson, Shane. R.. University of London; Reino Unido
Fil: Tekwani, Babu L.. University of Mississippi; Estados Unidos
Fil: Labadie, Guillermo Roberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
description A series of 25 N,N-substituted diamines were prepared by controlled reductive amination of free aliphatic diamines with different substituted benzaldehydes. The library was screened in vitro for antiparasitic activity on the causative agents of human African trypanosomiasis, Chagas’ disease and visceral leishmaniasis. The most potent compounds were derived from a subset of diamines that contained a 4-OBn substitution, having a 50% parasite growth inhibition in the submicromolar (against Trypanosoma cruzi) or nanomolar (against Trypanosoma brucei and Leishmania donovani) range. We conclude that members of this series of N,N´-substituted diamines provide new lead structures that have potential to treat trypanosomal and leishmanial infections.
publishDate 2012
dc.date.none.fl_str_mv 2012-02-15
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/11336/111686
Caminos, Andrea P.; Panozzo Zenere, Esteban Andrés; Wilkinson, Shane. R.; Tekwani, Babu L.; Labadie, Guillermo Roberto; Synthesis and antikinetoplastid activity of a series of N,N′-substituted diamines; Pergamon-Elsevier Science Ltd; Bioorganic & Medicinal Chemistry Letters; 22; 4; 15-2-2012; 1712-1715
0960-894X
CONICET Digital
CONICET
url http://hdl.handle.net/11336/111686
identifier_str_mv Caminos, Andrea P.; Panozzo Zenere, Esteban Andrés; Wilkinson, Shane. R.; Tekwani, Babu L.; Labadie, Guillermo Roberto; Synthesis and antikinetoplastid activity of a series of N,N′-substituted diamines; Pergamon-Elsevier Science Ltd; Bioorganic & Medicinal Chemistry Letters; 22; 4; 15-2-2012; 1712-1715
0960-894X
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Corregido en https://doi.org/10.1016/j.bmcl.2013.02.003
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.bmcl.2011.12.101
info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/abs/pii/S0960894X11017835
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
dc.publisher.none.fl_str_mv Pergamon-Elsevier Science Ltd
publisher.none.fl_str_mv Pergamon-Elsevier Science Ltd
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
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
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score 12.993085

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