Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2
| Autor(a) principal: | |
|---|---|
| Data de Publicação: | 2009 |
| Outros Autores: | , , , , , , , , , , |
| Tipo de documento: | Artigo |
| Idioma: | eng |
| Título da fonte: | Repositório Institucional da FIOCRUZ (ARCA) |
| DOI: | 10.1016/j.ejmech.2009.03.041 |
| Texto Completo: | https://www.arca.fiocruz.br/handle/icict/34841 |
Resumo: | 2020-08-15 |
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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 |
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2020-08-15 |
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2009 |
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2009 |
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2019-08-15T19:22:29Z |
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2019-08-15T19:22:29Z |
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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. |
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0223-5234 |
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10.1016/j.ejmech.2009.03.041 |
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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 |
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