3-alcoxi-4-hidroxi pirrolidin-2-onas, 2-metilsulfanil pirimidina, enoilcarbamatos e 3-dialcoxi fosforiloxi trialometilados: síntese e potencial inibitório sobre a atividade da enzima acetilcolinesterase

Detalhes bibliográficos
Autor(a) principal: Obregon, Adriana Dornelles Carpes
Data de Publicação: 2006
Tipo de documento: Tese
Idioma: por
Título da fonte: Manancial - Repositório Digital da UFSM
dARK ID: ark:/26339/001300000nc1n
Texto Completo: http://repositorio.ufsm.br/handle/1/4239
Resumo: This work presents a study of the several organic compounds such as trihalomethylated enaminones, γ-amino alcohols, oxazinones, oxazines, dihydrofuranones, pyrrolidin-2-ones, 2-methylsulfanyl pyrimidine, enoylcarbamates and 3-dialkoxy phosphoryloxy on the acetylcholinesterase enzyme activity. Also, this work shows the effect per se of organic solvents on the AChE of different cerebral structures of rats. The N- and N-O-alkylated 3-alkoxy-5-hydroxy-trifluormethyl-pyrrolidin-2-ones and trifluoromethylated enoylcarbamates showed in vitro inhibitory effect of the AChE activity in the striatum cerebral of rat, at the concentration 1.0 mM. The dimethyl-[(2-methylsulfanyl-4-trichloromethyl-6-pyrimidin-ylmethoxy)-ethyl] amine showed significant inhibitory effect (p<0.001) in vitro on AChE activity of the striatum cerebral of rat, in the concentration 0.1mM. The in vivo effect of this pyrimidine was significant (p<0.001) in the concentration of 10mg/Kg in the AChE activity in striatum and erythrocyte of rat. Finally, the trifluoromethylated 3-diethoxy-phosphoryloxy ethyl carbamates show significant inhibitory effect (p<0.001) on the purified AChE activity at the concentration of 0.001 mM.
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spelling 3-alcoxi-4-hidroxi pirrolidin-2-onas, 2-metilsulfanil pirimidina, enoilcarbamatos e 3-dialcoxi fosforiloxi trialometilados: síntese e potencial inibitório sobre a atividade da enzima acetilcolinesteraseTrihalomethylated 3-alkoxy-4-hydroxy pyrrolidin-2-ones, 2-methylsulfanyl pyrimidine, enoylcarbamates and 3-dialkoxy phosphoryloxy: synthesis and potential inhibitory activity on the acetylcholinesterase enzymeQuímica orgânicaCompostos orgânicosEnzimasCNPQ::CIENCIAS EXATAS E DA TERRA::QUIMICAThis work presents a study of the several organic compounds such as trihalomethylated enaminones, γ-amino alcohols, oxazinones, oxazines, dihydrofuranones, pyrrolidin-2-ones, 2-methylsulfanyl pyrimidine, enoylcarbamates and 3-dialkoxy phosphoryloxy on the acetylcholinesterase enzyme activity. Also, this work shows the effect per se of organic solvents on the AChE of different cerebral structures of rats. The N- and N-O-alkylated 3-alkoxy-5-hydroxy-trifluormethyl-pyrrolidin-2-ones and trifluoromethylated enoylcarbamates showed in vitro inhibitory effect of the AChE activity in the striatum cerebral of rat, at the concentration 1.0 mM. The dimethyl-[(2-methylsulfanyl-4-trichloromethyl-6-pyrimidin-ylmethoxy)-ethyl] amine showed significant inhibitory effect (p<0.001) in vitro on AChE activity of the striatum cerebral of rat, in the concentration 0.1mM. The in vivo effect of this pyrimidine was significant (p<0.001) in the concentration of 10mg/Kg in the AChE activity in striatum and erythrocyte of rat. Finally, the trifluoromethylated 3-diethoxy-phosphoryloxy ethyl carbamates show significant inhibitory effect (p<0.001) on the purified AChE activity at the concentration of 0.001 mM.Este trabalho apresenta um estudo de várias classes de compostos orgânicos: enamino compostos, γ-aminoálcoois, oxazinonas, oxazinas, diidrofuranonas, pirrolidin-2-onas, 2-metilsulfanil pirimidina, enoilcarbamatos e 3-dialcoxi fosforiloxi trialometilados sobre a atividade da enzima acetilcolinesterase. Também demonstra o efeito per se de solventes orgânicos sobre a atividade da AChE em diferentes estruturas cerebrais de rato. As 3-alcoxi-5-hidroxi-5-trifluormetil pirrolidin-2-onas N-alquiladas e N-O-alquiladas e os enoilcarbamatos trifluormetilados mostraram efeito inibitório significativo (p<0,05) sobre a atividade in vitro da AChE de estriado cerebral de rato, na concentração de 1,0 mM. A dimetil-(2-metilsulfanil-4-triclorometil-6-pirimidinilme-toxi)etil] amina mostrou efeito inibitório significativo (p<0,001) sobre a atividade in vitro da AChE de estriado cerebral de rato na concentração de 0,1mM. O efeito in vivo dessa pirimidina foi significativo (p<0,001) na concentração de 10 mg/Kg sobre a atividade da AChE em estriado cerebral e membrana de eritrócitos de rato. Finalmente, as 3-dietoxi-fosforiloxi carbamatos de etila trifluormetilados mostraram efeito inibitório significativo (p<0.001) sobre a atividade da AChE purificada em concentrações a partir de 0.001 mM.Universidade Federal de Santa MariaBRQuímicaUFSMPrograma de Pós-Graduação em QuímicaZanatta, Nilohttp://lattes.cnpq.br/0719465062354576Schetinger, Maria Rosa ChitolinaBonan, Carla Denisehttp://lattes.cnpq.br/8058052532279136Bonacorso, Helio Gauzehttp://lattes.cnpq.br/7275608974248322Dalcol, Ionara Irionhttp://lattes.cnpq.br/9769548819312192Obregon, Adriana Dornelles Carpes2017-05-102017-05-102006-10-20info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/doctoralThesisapplication/pdfapplication/pdfOBREGON, Adriana Dornelles Carpes. Trihalomethylated 3-alkoxy-4-hydroxy pyrrolidin-2-ones, 2-methylsulfanyl pyrimidine, enoylcarbamates and 3-dialkoxy phosphoryloxy: synthesis and potential inhibitory activity on the acetylcholinesterase enzyme. 2006. 130 f. Tese (Doutorado em Química) - Universidade Federal de Santa Maria, Santa Maria, 2006.http://repositorio.ufsm.br/handle/1/4239ark:/26339/001300000nc1nporinfo:eu-repo/semantics/openAccessreponame:Manancial - Repositório Digital da UFSMinstname:Universidade Federal de Santa Maria (UFSM)instacron:UFSM2022-07-21T17:56:46Zoai:repositorio.ufsm.br:1/4239Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufsm.br/ONGhttps://repositorio.ufsm.br/oai/requestatendimento.sib@ufsm.br||tedebc@gmail.comopendoar:2022-07-21T17:56:46Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)false
dc.title.none.fl_str_mv 3-alcoxi-4-hidroxi pirrolidin-2-onas, 2-metilsulfanil pirimidina, enoilcarbamatos e 3-dialcoxi fosforiloxi trialometilados: síntese e potencial inibitório sobre a atividade da enzima acetilcolinesterase
Trihalomethylated 3-alkoxy-4-hydroxy pyrrolidin-2-ones, 2-methylsulfanyl pyrimidine, enoylcarbamates and 3-dialkoxy phosphoryloxy: synthesis and potential inhibitory activity on the acetylcholinesterase enzyme
title 3-alcoxi-4-hidroxi pirrolidin-2-onas, 2-metilsulfanil pirimidina, enoilcarbamatos e 3-dialcoxi fosforiloxi trialometilados: síntese e potencial inibitório sobre a atividade da enzima acetilcolinesterase
spellingShingle 3-alcoxi-4-hidroxi pirrolidin-2-onas, 2-metilsulfanil pirimidina, enoilcarbamatos e 3-dialcoxi fosforiloxi trialometilados: síntese e potencial inibitório sobre a atividade da enzima acetilcolinesterase
Obregon, Adriana Dornelles Carpes
Química orgânica
Compostos orgânicos
Enzimas
CNPQ::CIENCIAS EXATAS E DA TERRA::QUIMICA
title_short 3-alcoxi-4-hidroxi pirrolidin-2-onas, 2-metilsulfanil pirimidina, enoilcarbamatos e 3-dialcoxi fosforiloxi trialometilados: síntese e potencial inibitório sobre a atividade da enzima acetilcolinesterase
title_full 3-alcoxi-4-hidroxi pirrolidin-2-onas, 2-metilsulfanil pirimidina, enoilcarbamatos e 3-dialcoxi fosforiloxi trialometilados: síntese e potencial inibitório sobre a atividade da enzima acetilcolinesterase
title_fullStr 3-alcoxi-4-hidroxi pirrolidin-2-onas, 2-metilsulfanil pirimidina, enoilcarbamatos e 3-dialcoxi fosforiloxi trialometilados: síntese e potencial inibitório sobre a atividade da enzima acetilcolinesterase
title_full_unstemmed 3-alcoxi-4-hidroxi pirrolidin-2-onas, 2-metilsulfanil pirimidina, enoilcarbamatos e 3-dialcoxi fosforiloxi trialometilados: síntese e potencial inibitório sobre a atividade da enzima acetilcolinesterase
title_sort 3-alcoxi-4-hidroxi pirrolidin-2-onas, 2-metilsulfanil pirimidina, enoilcarbamatos e 3-dialcoxi fosforiloxi trialometilados: síntese e potencial inibitório sobre a atividade da enzima acetilcolinesterase
author Obregon, Adriana Dornelles Carpes
author_facet Obregon, Adriana Dornelles Carpes
author_role author
dc.contributor.none.fl_str_mv Zanatta, Nilo
http://lattes.cnpq.br/0719465062354576
Schetinger, Maria Rosa Chitolina
Bonan, Carla Denise
http://lattes.cnpq.br/8058052532279136
Bonacorso, Helio Gauze
http://lattes.cnpq.br/7275608974248322
Dalcol, Ionara Irion
http://lattes.cnpq.br/9769548819312192
dc.contributor.author.fl_str_mv Obregon, Adriana Dornelles Carpes
dc.subject.por.fl_str_mv Química orgânica
Compostos orgânicos
Enzimas
CNPQ::CIENCIAS EXATAS E DA TERRA::QUIMICA
topic Química orgânica
Compostos orgânicos
Enzimas
CNPQ::CIENCIAS EXATAS E DA TERRA::QUIMICA
description This work presents a study of the several organic compounds such as trihalomethylated enaminones, γ-amino alcohols, oxazinones, oxazines, dihydrofuranones, pyrrolidin-2-ones, 2-methylsulfanyl pyrimidine, enoylcarbamates and 3-dialkoxy phosphoryloxy on the acetylcholinesterase enzyme activity. Also, this work shows the effect per se of organic solvents on the AChE of different cerebral structures of rats. The N- and N-O-alkylated 3-alkoxy-5-hydroxy-trifluormethyl-pyrrolidin-2-ones and trifluoromethylated enoylcarbamates showed in vitro inhibitory effect of the AChE activity in the striatum cerebral of rat, at the concentration 1.0 mM. The dimethyl-[(2-methylsulfanyl-4-trichloromethyl-6-pyrimidin-ylmethoxy)-ethyl] amine showed significant inhibitory effect (p<0.001) in vitro on AChE activity of the striatum cerebral of rat, in the concentration 0.1mM. The in vivo effect of this pyrimidine was significant (p<0.001) in the concentration of 10mg/Kg in the AChE activity in striatum and erythrocyte of rat. Finally, the trifluoromethylated 3-diethoxy-phosphoryloxy ethyl carbamates show significant inhibitory effect (p<0.001) on the purified AChE activity at the concentration of 0.001 mM.
publishDate 2006
dc.date.none.fl_str_mv 2006-10-20
2017-05-10
2017-05-10
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/doctoralThesis
format doctoralThesis
status_str publishedVersion
dc.identifier.uri.fl_str_mv OBREGON, Adriana Dornelles Carpes. Trihalomethylated 3-alkoxy-4-hydroxy pyrrolidin-2-ones, 2-methylsulfanyl pyrimidine, enoylcarbamates and 3-dialkoxy phosphoryloxy: synthesis and potential inhibitory activity on the acetylcholinesterase enzyme. 2006. 130 f. Tese (Doutorado em Química) - Universidade Federal de Santa Maria, Santa Maria, 2006.
http://repositorio.ufsm.br/handle/1/4239
dc.identifier.dark.fl_str_mv ark:/26339/001300000nc1n
identifier_str_mv OBREGON, Adriana Dornelles Carpes. Trihalomethylated 3-alkoxy-4-hydroxy pyrrolidin-2-ones, 2-methylsulfanyl pyrimidine, enoylcarbamates and 3-dialkoxy phosphoryloxy: synthesis and potential inhibitory activity on the acetylcholinesterase enzyme. 2006. 130 f. Tese (Doutorado em Química) - Universidade Federal de Santa Maria, Santa Maria, 2006.
ark:/26339/001300000nc1n
url http://repositorio.ufsm.br/handle/1/4239
dc.language.iso.fl_str_mv por
language por
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Universidade Federal de Santa Maria
BR
Química
UFSM
Programa de Pós-Graduação em Química
publisher.none.fl_str_mv Universidade Federal de Santa Maria
BR
Química
UFSM
Programa de Pós-Graduação em Química
dc.source.none.fl_str_mv reponame:Manancial - Repositório Digital da UFSM
instname:Universidade Federal de Santa Maria (UFSM)
instacron:UFSM
instname_str Universidade Federal de Santa Maria (UFSM)
instacron_str UFSM
institution UFSM
reponame_str Manancial - Repositório Digital da UFSM
collection Manancial - Repositório Digital da UFSM
repository.name.fl_str_mv Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)
repository.mail.fl_str_mv atendimento.sib@ufsm.br||tedebc@gmail.com
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