Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2

Bibliographic Details
Main Author: Cunico, Wilson
Publication Date: 2009
Other Authors: Gomes, Claudia Regina Brandão, Facchinetti, Victor, Moreth, Marcele, Penido, Carmen, Henriques, Maria das Graças Muller Oliveira, Varotti, Fernando Pilla, Krettli, Luisa Guimarães, Krettli, Antoniana Ursine, da Silva, Franklin Souza, Caffarena, Ernesto Raúl, Silveira, Camila Magalhães
Format: Article
Language: eng
Source: Repositório Institucional da FIOCRUZ (ARCA)
Download full: https://www.arca.fiocruz.br/handle/icict/34841
Summary: 2020-08-15
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spelling Cunico, WilsonGomes, Claudia Regina BrandãoFacchinetti, VictorMoreth, MarcelePenido, CarmenHenriques, Maria das Graças Muller OliveiraVarotti, Fernando PillaKrettli, Luisa GuimarãesKrettli, Antoniana Ursineda Silva, Franklin SouzaCaffarena, Ernesto RaúlSilveira, Camila Magalhães2019-08-15T19:22:29Z2019-08-15T19:22:29Z2009CUNICO, Wilson et al. Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, Part 2. European Journal of Medicinal Chemistry, v. 44, n. 9, p. 3816-3820, Sept. 2009.0223-5234https://www.arca.fiocruz.br/handle/icict/3484110.1016/j.ejmech.2009.03.041engElsevierInibidor de ProteaseMaláriaHidroxietilaminaProtease InhibitorMalariaHydroxyethylamineSynthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article2020-08-15Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Departamento de Síntese. Rio de Janeiro, RJ, Brasil / Universidade Federal de Pelotas. Departamento de Química Orgânica. Pelotas, RS, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Departamento de Síntese. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Departamento de Síntese. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Departamento de Síntese. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Departamento de Farmacologia Aplicada. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Departamento de Farmacologia Aplicada. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Malária. Belo Horizonte, MG, Brasil / Universidade Federal de Minas Gerais. Programa de Farmacologia Bioquímica e Molecular. Belo Horizonte, MG, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Malária. Belo Horizonte, MG, Brasil.Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Malária. Belo Horizonte, MG, Brasil / Universidade Federal de Minas Gerais. Programa de Farmacologia Bioquímica e Molecular. Belo Horizonte, MG, Brasil.Fundação Oswaldo Cruz. Presidência. Programa de Computação Científica. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Presidência. Programa de Computação Científica. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Presidência. Programa de Computação Científica. Rio de Janeiro, RJ, Brasil.The antimalarial acitivity of hydroxyethylamines, synthesized from the reaction of intermediated hydroxyethypiperazines with benzenesulfonyl chlorides or benzoyl chlorides, has been evaluated in vitro against a W2 Plasmodium falciparum clone. Some of the nineteen tested derivatives showed a significant activity in vitro, thus turning into a promising new class of antimalarials. In addition, a molecular modeling study of the most active derivative (5l) was performed and its most probable binding modes within plasmepsin II enzyme were identified.info:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZORIGINALSynthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, Part 2.pdfSynthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, Part 2.pdfapplication/pdf3025973https://www.arca.fiocruz.br/bitstream/icict/34841/1/Synthesis%2c%20antimalarial%20evaluation%20and%20molecular%20modeling%20studies%20of%20hydroxyethylpiperazines%2c%20potential%20aspartyl%20protease%20inhibitors%2c%20Part%202.pdf61a594708f5386d498f3d7a68d8efe8cMD51TEXTSynthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, Part 2.pdf.txtSynthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, Part 2.pdf.txtExtracted texttext/plain5https://www.arca.fiocruz.br/bitstream/icict/34841/2/Synthesis%2c%20antimalarial%20evaluation%20and%20molecular%20modeling%20studies%20of%20hydroxyethylpiperazines%2c%20potential%20aspartyl%20protease%20inhibitors%2c%20Part%202.pdf.txtcc9067c2ee470dc248b14b194209a34eMD52icict/348412021-03-24 16:32:35.31oai:www.arca.fiocruz.br:icict/34841Repositório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352021-03-24T19:32:35Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false
dc.title.pt_BR.fl_str_mv Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2
title Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2
spellingShingle Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2
Cunico, Wilson
Inibidor de Protease
Malária
Hidroxietilamina
Protease Inhibitor
Malaria
Hydroxyethylamine
title_short Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2
title_full Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2
title_fullStr Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2
title_full_unstemmed Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2
title_sort Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2
author Cunico, Wilson
author_facet Cunico, Wilson
Gomes, Claudia Regina Brandão
Facchinetti, Victor
Moreth, Marcele
Penido, Carmen
Henriques, Maria das Graças Muller Oliveira
Varotti, Fernando Pilla
Krettli, Luisa Guimarães
Krettli, Antoniana Ursine
da Silva, Franklin Souza
Caffarena, Ernesto Raúl
Silveira, Camila Magalhães
author_role author
author2 Gomes, Claudia Regina Brandão
Facchinetti, Victor
Moreth, Marcele
Penido, Carmen
Henriques, Maria das Graças Muller Oliveira
Varotti, Fernando Pilla
Krettli, Luisa Guimarães
Krettli, Antoniana Ursine
da Silva, Franklin Souza
Caffarena, Ernesto Raúl
Silveira, Camila Magalhães
author2_role author
author
author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Cunico, Wilson
Gomes, Claudia Regina Brandão
Facchinetti, Victor
Moreth, Marcele
Penido, Carmen
Henriques, Maria das Graças Muller Oliveira
Varotti, Fernando Pilla
Krettli, Luisa Guimarães
Krettli, Antoniana Ursine
da Silva, Franklin Souza
Caffarena, Ernesto Raúl
Silveira, Camila Magalhães
dc.subject.other.pt_BR.fl_str_mv Inibidor de Protease
Malária
Hidroxietilamina
topic Inibidor de Protease
Malária
Hidroxietilamina
Protease Inhibitor
Malaria
Hydroxyethylamine
dc.subject.en.pt_BR.fl_str_mv Protease Inhibitor
Malaria
Hydroxyethylamine
description 2020-08-15
publishDate 2009
dc.date.issued.fl_str_mv 2009
dc.date.accessioned.fl_str_mv 2019-08-15T19:22:29Z
dc.date.available.fl_str_mv 2019-08-15T19:22:29Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.citation.fl_str_mv CUNICO, Wilson et al. Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, Part 2. European Journal of Medicinal Chemistry, v. 44, n. 9, p. 3816-3820, Sept. 2009.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/34841
dc.identifier.issn.pt_BR.fl_str_mv 0223-5234
dc.identifier.doi.none.fl_str_mv 10.1016/j.ejmech.2009.03.041
identifier_str_mv CUNICO, Wilson et al. Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, Part 2. European Journal of Medicinal Chemistry, v. 44, n. 9, p. 3816-3820, Sept. 2009.
0223-5234
10.1016/j.ejmech.2009.03.041
url https://www.arca.fiocruz.br/handle/icict/34841
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
instname:Fundação Oswaldo Cruz (FIOCRUZ)
instacron:FIOCRUZ
instname_str Fundação Oswaldo Cruz (FIOCRUZ)
instacron_str FIOCRUZ
institution FIOCRUZ
reponame_str Repositório Institucional da FIOCRUZ (ARCA)
collection Repositório Institucional da FIOCRUZ (ARCA)
bitstream.url.fl_str_mv https://www.arca.fiocruz.br/bitstream/icict/34841/1/Synthesis%2c%20antimalarial%20evaluation%20and%20molecular%20modeling%20studies%20of%20hydroxyethylpiperazines%2c%20potential%20aspartyl%20protease%20inhibitors%2c%20Part%202.pdf
https://www.arca.fiocruz.br/bitstream/icict/34841/2/Synthesis%2c%20antimalarial%20evaluation%20and%20molecular%20modeling%20studies%20of%20hydroxyethylpiperazines%2c%20potential%20aspartyl%20protease%20inhibitors%2c%20Part%202.pdf.txt
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repository.name.fl_str_mv Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)
repository.mail.fl_str_mv repositorio.arca@fiocruz.br
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