Síntese de novos fosforamidatos com avitidades ani-HSV-1

Detalhes bibliográficos
Autor(a) principal: Macedo, William Pires de
Data de Publicação: 2007
Tipo de documento: Tese
Idioma: por
Título da fonte: Repositório Institucional da Universidade Federal Fluminense (RIUFF)
Texto Completo: https://app.uff.br/riuff/handle/1/17982
Resumo: The number of the phosphoramidic acid derivatives associated with molecular systems of known biological activity is growing significantly. This is attributed, mainly, to the stability that the compound acquires in physiological environment, when it is incorporated into a phosphoramidic group, toward different enzymatic systems, like the nucleases. Based on a novel antiviral therapeutic concept, an efficient technique was developed, by which phosphoramidic groups are connected to heterocyclic systems with renowned biological activity, after modifications of known methodology for similar reactions. Herein, heterocyclic substrates such as 4-chloro-pirazolo[3,4-b]pyridine, 4-chloro-quinoline and 4-choloro-thieno[2,3-b]pyridine were phosphorylated by aminoalkyl phosphoramidic acid esters, generating three new phosphoramidate derivatives of series 60, 61 and 62,respectively.The products of the three series were obtained in good yield and tested against HSV-1 virus.
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spelling Síntese de novos fosforamidatos com avitidades ani-HSV-1Synthesis of new fosforamidatos anti-HSV-1Ácido fosforamídicoFosforamidatosAnti-HSV-1Phosphoramidic acidPhosphoramidatesAni-HSV-1CNPQ::CIENCIAS EXATAS E DA TERRA::QUIMICAThe number of the phosphoramidic acid derivatives associated with molecular systems of known biological activity is growing significantly. This is attributed, mainly, to the stability that the compound acquires in physiological environment, when it is incorporated into a phosphoramidic group, toward different enzymatic systems, like the nucleases. Based on a novel antiviral therapeutic concept, an efficient technique was developed, by which phosphoramidic groups are connected to heterocyclic systems with renowned biological activity, after modifications of known methodology for similar reactions. Herein, heterocyclic substrates such as 4-chloro-pirazolo[3,4-b]pyridine, 4-chloro-quinoline and 4-choloro-thieno[2,3-b]pyridine were phosphorylated by aminoalkyl phosphoramidic acid esters, generating three new phosphoramidate derivatives of series 60, 61 and 62,respectively.The products of the three series were obtained in good yield and tested against HSV-1 virus.Coordenação de Aperfeiçoamento de Pessoal de Nível SuperiorO número de derivados do ácido fosforamídico associados com sistemas moleculares de reconhecida atividade biológica vem aumentado significativamente. Isto se deve, principalmente, à estabilidade que o composto adquire no meio fisiológico, quando incorporado ao grupamento fosforamídico, principalmente frente aos vários sistemas enzimáticos, como as nucleases. Baseado em um novo conceito terapêutico antiviral, desenvolveu-se uma técnica eficiente de inserção de grupamentos fosforamidato em sistemas heterocíclicos com reconhecida atividade biológica, a partir de modificações em metodologia conhecida para reações análogas. Neste trabalho desenvolveu-se novos fosforamidatos com substituintes heterociclicos derivados dos sistemas pirazolo[3,4-b]piridina (60), quinolina (61) e tieno[2,3- b]piridina (62).Os produtos das séries 60(a-m), 61(a-d) (e-g) (i-m) (n-q) (r-u) e 62a-c foram obtidos com bons rendimentos. Nota do catalogador: O resumo inclui imagens que não foram inseridas.Programa de Pós-graduação em Química OrgânicaQuímica OrgânicaSouza, Marcos Costa deCPF:98897007960http://genos.cnpq.br:12010/dwlattes/owa/prc_imp_cv_int?f_cod=K4785064D6Bernardino, Alice Maria RolimCPF:36505404791http://lattes.cnpq.br/6370709289392476Frugulhetti, Izabel Christina de Palmer PaixaoCPF:46322264753http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4783557Z4Cunha, Maria Fernanda Vasconcelos daCPF:58787585787http://genos.cnpq.br:12010/dwlattes/owa/prc_imp_cv_int?f_cod=K4786691Y5Lin, Whei OhCPF:77666555522http://lattes.cnpq.br/4147267117931858Costa, João Batista Neves daCPF:89989898922http://lattes.cnpq.br/8678051184959173Macedo, William Pires de2021-03-10T20:43:16Z2008-11-072021-03-10T20:43:16Z2007-02-27info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/doctoralThesisapplication/pdfhttps://app.uff.br/riuff/handle/1/17982porCC-BY-SAinfo:eu-repo/semantics/embargoedAccessreponame:Repositório Institucional da Universidade Federal Fluminense (RIUFF)instname:Universidade Federal Fluminense (UFF)instacron:UFF2021-03-10T20:43:16Zoai:app.uff.br:1/17982Repositório InstitucionalPUBhttps://app.uff.br/oai/requestriuff@id.uff.bropendoar:21202021-03-10T20:43:16Repositório Institucional da Universidade Federal Fluminense (RIUFF) - Universidade Federal Fluminense (UFF)false
dc.title.none.fl_str_mv Síntese de novos fosforamidatos com avitidades ani-HSV-1
Synthesis of new fosforamidatos anti-HSV-1
title Síntese de novos fosforamidatos com avitidades ani-HSV-1
spellingShingle Síntese de novos fosforamidatos com avitidades ani-HSV-1
Macedo, William Pires de
Ácido fosforamídico
Fosforamidatos
Anti-HSV-1
Phosphoramidic acid
Phosphoramidates
Ani-HSV-1
CNPQ::CIENCIAS EXATAS E DA TERRA::QUIMICA
title_short Síntese de novos fosforamidatos com avitidades ani-HSV-1
title_full Síntese de novos fosforamidatos com avitidades ani-HSV-1
title_fullStr Síntese de novos fosforamidatos com avitidades ani-HSV-1
title_full_unstemmed Síntese de novos fosforamidatos com avitidades ani-HSV-1
title_sort Síntese de novos fosforamidatos com avitidades ani-HSV-1
author Macedo, William Pires de
author_facet Macedo, William Pires de
author_role author
dc.contributor.none.fl_str_mv Souza, Marcos Costa de
CPF:98897007960
http://genos.cnpq.br:12010/dwlattes/owa/prc_imp_cv_int?f_cod=K4785064D6
Bernardino, Alice Maria Rolim
CPF:36505404791
http://lattes.cnpq.br/6370709289392476
Frugulhetti, Izabel Christina de Palmer Paixao
CPF:46322264753
http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4783557Z4
Cunha, Maria Fernanda Vasconcelos da
CPF:58787585787
http://genos.cnpq.br:12010/dwlattes/owa/prc_imp_cv_int?f_cod=K4786691Y5
Lin, Whei Oh
CPF:77666555522
http://lattes.cnpq.br/4147267117931858
Costa, João Batista Neves da
CPF:89989898922
http://lattes.cnpq.br/8678051184959173
dc.contributor.author.fl_str_mv Macedo, William Pires de
dc.subject.por.fl_str_mv Ácido fosforamídico
Fosforamidatos
Anti-HSV-1
Phosphoramidic acid
Phosphoramidates
Ani-HSV-1
CNPQ::CIENCIAS EXATAS E DA TERRA::QUIMICA
topic Ácido fosforamídico
Fosforamidatos
Anti-HSV-1
Phosphoramidic acid
Phosphoramidates
Ani-HSV-1
CNPQ::CIENCIAS EXATAS E DA TERRA::QUIMICA
description The number of the phosphoramidic acid derivatives associated with molecular systems of known biological activity is growing significantly. This is attributed, mainly, to the stability that the compound acquires in physiological environment, when it is incorporated into a phosphoramidic group, toward different enzymatic systems, like the nucleases. Based on a novel antiviral therapeutic concept, an efficient technique was developed, by which phosphoramidic groups are connected to heterocyclic systems with renowned biological activity, after modifications of known methodology for similar reactions. Herein, heterocyclic substrates such as 4-chloro-pirazolo[3,4-b]pyridine, 4-chloro-quinoline and 4-choloro-thieno[2,3-b]pyridine were phosphorylated by aminoalkyl phosphoramidic acid esters, generating three new phosphoramidate derivatives of series 60, 61 and 62,respectively.The products of the three series were obtained in good yield and tested against HSV-1 virus.
publishDate 2007
dc.date.none.fl_str_mv 2007-02-27
2008-11-07
2021-03-10T20:43:16Z
2021-03-10T20:43:16Z
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 https://app.uff.br/riuff/handle/1/17982
url https://app.uff.br/riuff/handle/1/17982
dc.language.iso.fl_str_mv por
language por
dc.rights.driver.fl_str_mv CC-BY-SA
info:eu-repo/semantics/embargoedAccess
rights_invalid_str_mv CC-BY-SA
eu_rights_str_mv embargoedAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Programa de Pós-graduação em Química Orgânica
Química Orgânica
publisher.none.fl_str_mv Programa de Pós-graduação em Química Orgânica
Química Orgânica
dc.source.none.fl_str_mv reponame:Repositório Institucional da Universidade Federal Fluminense (RIUFF)
instname:Universidade Federal Fluminense (UFF)
instacron:UFF
instname_str Universidade Federal Fluminense (UFF)
instacron_str UFF
institution UFF
reponame_str Repositório Institucional da Universidade Federal Fluminense (RIUFF)
collection Repositório Institucional da Universidade Federal Fluminense (RIUFF)
repository.name.fl_str_mv Repositório Institucional da Universidade Federal Fluminense (RIUFF) - Universidade Federal Fluminense (UFF)
repository.mail.fl_str_mv riuff@id.uff.br
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