Síntese de novos fosforamidatos com avitidades ani-HSV-1
Autor(a) principal: | |
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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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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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1807838743140237312 |