Microwave-assisted synthesis and pharmacological screening of some triazolothiadiazole derivatives
Autor(a) principal: | |
---|---|
Data de Publicação: | 2020 |
Outros Autores: | , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Brazilian Journal of Pharmaceutical Sciences |
Texto Completo: | https://www.revistas.usp.br/bjps/article/view/181437 |
Resumo: | In this study, twenty-two new [1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles (5a-n, 6a-h) were synthesized under microwave irradiation (MWI). The chemical structures of the compounds were elucidated by their IR, 1 H-NMR, LC-MS, and elemental analysis. The compounds were tested for antinociceptive activity by using the tail clip, tail flick, hot plate, and writhing methods in mice. The varying levels of antinociceptive activity of the compounds were compared with those of aspirin. Among these compounds, compound 5g and 5j were found to be significantly more active than the other compounds and the standard in the tests. Also, inhibitory effects of the test compounds on COX-1 and COX-2 activities were investigated. DuP-697 for COX-2 and SC-560 for COX-1 were used as reference standards. |
id |
USP-31_77c2b9891363e411fa0cfcbc24da78d1 |
---|---|
oai_identifier_str |
oai:revistas.usp.br:article/181437 |
network_acronym_str |
USP-31 |
network_name_str |
Brazilian Journal of Pharmaceutical Sciences |
repository_id_str |
|
spelling |
Microwave-assisted synthesis and pharmacological screening of some triazolothiadiazole derivatives2(3H)-BenzoxazoloneTriazolothiadiazoleAntinociceptive activityMicrowave-assisted synthesisIn this study, twenty-two new [1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles (5a-n, 6a-h) were synthesized under microwave irradiation (MWI). The chemical structures of the compounds were elucidated by their IR, 1 H-NMR, LC-MS, and elemental analysis. The compounds were tested for antinociceptive activity by using the tail clip, tail flick, hot plate, and writhing methods in mice. The varying levels of antinociceptive activity of the compounds were compared with those of aspirin. Among these compounds, compound 5g and 5j were found to be significantly more active than the other compounds and the standard in the tests. Also, inhibitory effects of the test compounds on COX-1 and COX-2 activities were investigated. DuP-697 for COX-2 and SC-560 for COX-1 were used as reference standards.Universidade de São Paulo. Faculdade de Ciências Farmacêuticas2020-12-09info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://www.revistas.usp.br/bjps/article/view/18143710.1590/s2175-97902019000318111Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18111Brazilian Journal of Pharmaceutical Sciences; v. 56 (2020); e18111Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e181112175-97901984-8250reponame:Brazilian Journal of Pharmaceutical Sciencesinstname:Universidade de São Paulo (USP)instacron:USPenghttps://www.revistas.usp.br/bjps/article/view/181437/168373Copyright (c) 2020 Brazilian Journal of Pharmaceutical Scienceshttp://creativecommons.org/licenses/by/4.0info:eu-repo/semantics/openAccessGorgu, Ozge Yıldırım, Engin Ozkan, Yesim Cakır, Bilge Erol, Kevser Onkol, Tijen 2021-06-12T19:46:54Zoai:revistas.usp.br:article/181437Revistahttps://www.revistas.usp.br/bjps/indexPUBhttps://old.scielo.br/oai/scielo-oai.phpbjps@usp.br||elizabeth.igne@gmail.com2175-97901984-8250opendoar:2021-06-12T19:46:54Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)false |
dc.title.none.fl_str_mv |
Microwave-assisted synthesis and pharmacological screening of some triazolothiadiazole derivatives |
title |
Microwave-assisted synthesis and pharmacological screening of some triazolothiadiazole derivatives |
spellingShingle |
Microwave-assisted synthesis and pharmacological screening of some triazolothiadiazole derivatives Gorgu, Ozge 2(3H)-Benzoxazolone Triazolothiadiazole Antinociceptive activity Microwave-assisted synthesis |
title_short |
Microwave-assisted synthesis and pharmacological screening of some triazolothiadiazole derivatives |
title_full |
Microwave-assisted synthesis and pharmacological screening of some triazolothiadiazole derivatives |
title_fullStr |
Microwave-assisted synthesis and pharmacological screening of some triazolothiadiazole derivatives |
title_full_unstemmed |
Microwave-assisted synthesis and pharmacological screening of some triazolothiadiazole derivatives |
title_sort |
Microwave-assisted synthesis and pharmacological screening of some triazolothiadiazole derivatives |
author |
Gorgu, Ozge |
author_facet |
Gorgu, Ozge Yıldırım, Engin Ozkan, Yesim Cakır, Bilge Erol, Kevser Onkol, Tijen |
author_role |
author |
author2 |
Yıldırım, Engin Ozkan, Yesim Cakır, Bilge Erol, Kevser Onkol, Tijen |
author2_role |
author author author author author |
dc.contributor.author.fl_str_mv |
Gorgu, Ozge Yıldırım, Engin Ozkan, Yesim Cakır, Bilge Erol, Kevser Onkol, Tijen |
dc.subject.por.fl_str_mv |
2(3H)-Benzoxazolone Triazolothiadiazole Antinociceptive activity Microwave-assisted synthesis |
topic |
2(3H)-Benzoxazolone Triazolothiadiazole Antinociceptive activity Microwave-assisted synthesis |
description |
In this study, twenty-two new [1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles (5a-n, 6a-h) were synthesized under microwave irradiation (MWI). The chemical structures of the compounds were elucidated by their IR, 1 H-NMR, LC-MS, and elemental analysis. The compounds were tested for antinociceptive activity by using the tail clip, tail flick, hot plate, and writhing methods in mice. The varying levels of antinociceptive activity of the compounds were compared with those of aspirin. Among these compounds, compound 5g and 5j were found to be significantly more active than the other compounds and the standard in the tests. Also, inhibitory effects of the test compounds on COX-1 and COX-2 activities were investigated. DuP-697 for COX-2 and SC-560 for COX-1 were used as reference standards. |
publishDate |
2020 |
dc.date.none.fl_str_mv |
2020-12-09 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/181437 10.1590/s2175-97902019000318111 |
url |
https://www.revistas.usp.br/bjps/article/view/181437 |
identifier_str_mv |
10.1590/s2175-97902019000318111 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/181437/168373 |
dc.rights.driver.fl_str_mv |
Copyright (c) 2020 Brazilian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by/4.0 info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
Copyright (c) 2020 Brazilian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by/4.0 |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
dc.source.none.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18111 Brazilian Journal of Pharmaceutical Sciences; v. 56 (2020); e18111 Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18111 2175-9790 1984-8250 reponame:Brazilian Journal of Pharmaceutical Sciences instname:Universidade de São Paulo (USP) instacron:USP |
instname_str |
Universidade de São Paulo (USP) |
instacron_str |
USP |
institution |
USP |
reponame_str |
Brazilian Journal of Pharmaceutical Sciences |
collection |
Brazilian Journal of Pharmaceutical Sciences |
repository.name.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP) |
repository.mail.fl_str_mv |
bjps@usp.br||elizabeth.igne@gmail.com |
_version_ |
1800222915072884736 |