Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit
Autor(a) principal: | |
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Data de Publicação: | 2014 |
Outros Autores: | , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.3390/molecules19022089 http://hdl.handle.net/11449/113465 |
Resumo: | Nonsteroidal anti-inflammatory drugs (NSAIDs) 1-5 containing an N-acyl hydrazone subunit were prepared and their antiplatelet and antithrombotic activities assessed in vitro and in vivo. Compounds 1-5 inhibited the platelet aggregation induced by adenosine diphosphate and/or arachidonic acid, with inhibition rates of 18.0%-61.1% and 65.9%-87.3%, respectively. Compounds 1 and 5 were the most active compounds, inhibiting adenosine-diphosphate-induced platelet aggregation by 57.2% and 61.1%, respectively. The inhibitory rates for arachidonic-acid-induced platelet aggregation were similar for compound 2 (80.8%) and acetylsalicylic acid (ASA, 80%). After their oral administration to mice, compounds 1, 3, and 5 showed shorter mean bleeding times than ASA. Compounds 1 and 5 also protected against thromboembolic events, with survival rates of 40% and 33%, respectively, compared with 30% for ASA. In conclusion, these results indicate that these novel NSAIDs containing an NAH subunit may offer better antiplatelet and antithrombotic activities than ASA. |
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Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone SubunithydrazoneantiplateletantithromboticNSAIDsbleeding timeNonsteroidal anti-inflammatory drugs (NSAIDs) 1-5 containing an N-acyl hydrazone subunit were prepared and their antiplatelet and antithrombotic activities assessed in vitro and in vivo. Compounds 1-5 inhibited the platelet aggregation induced by adenosine diphosphate and/or arachidonic acid, with inhibition rates of 18.0%-61.1% and 65.9%-87.3%, respectively. Compounds 1 and 5 were the most active compounds, inhibiting adenosine-diphosphate-induced platelet aggregation by 57.2% and 61.1%, respectively. The inhibitory rates for arachidonic-acid-induced platelet aggregation were similar for compound 2 (80.8%) and acetylsalicylic acid (ASA, 80%). After their oral administration to mice, compounds 1, 3, and 5 showed shorter mean bleeding times than ASA. Compounds 1 and 5 also protected against thromboembolic events, with survival rates of 40% and 33%, respectively, compared with 30% for ASA. In conclusion, these results indicate that these novel NSAIDs containing an NAH subunit may offer better antiplatelet and antithrombotic activities than ASA.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)UNESP, Fac Ciencias Farmaceut, Dept Farmacos & Med, BR-14801902 Araraquara, SP, BrazilUNESP, Fac Ciencias Farmaceut, Dept Farmacos & Med, BR-14801902 Araraquara, SP, BrazilFAPESP: 11/15204-5FAPESP: 12/50359-2Mdpi AgUniversidade Estadual Paulista (Unesp)Chelucci, Rafael Consolin [UNESP]Dutra, Luiz Antonio [UNESP]Lopes Pires, Maria Elisa [UNESP]Ferreira de Melo, Thais Regina [UNESP]Bosquesi, Priscila Longhin [UNESP]Chin, Chung Man [UNESP]Santos, Jean Leandro dos [UNESP]2014-12-03T13:11:43Z2014-12-03T13:11:43Z2014-02-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article2089-2099application/pdfhttp://dx.doi.org/10.3390/molecules19022089Molecules. Basel: Mdpi Ag, v. 19, n. 2, p. 2089-2099, 2014.1420-3049http://hdl.handle.net/11449/11346510.3390/molecules19022089WOS:000334418200045WOS000334418200045.pdf97343336079754130000-0003-4141-0455Web of Sciencereponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengMolecules3.0980,855info:eu-repo/semantics/openAccess2024-06-24T13:46:24Zoai:repositorio.unesp.br:11449/113465Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T22:43:51.029713Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit |
title |
Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit |
spellingShingle |
Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit Chelucci, Rafael Consolin [UNESP] hydrazone antiplatelet antithrombotic NSAIDs bleeding time |
title_short |
Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit |
title_full |
Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit |
title_fullStr |
Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit |
title_full_unstemmed |
Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit |
title_sort |
Antiplatelet and Antithrombotic Activities of Non-Steroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit |
author |
Chelucci, Rafael Consolin [UNESP] |
author_facet |
Chelucci, Rafael Consolin [UNESP] Dutra, Luiz Antonio [UNESP] Lopes Pires, Maria Elisa [UNESP] Ferreira de Melo, Thais Regina [UNESP] Bosquesi, Priscila Longhin [UNESP] Chin, Chung Man [UNESP] Santos, Jean Leandro dos [UNESP] |
author_role |
author |
author2 |
Dutra, Luiz Antonio [UNESP] Lopes Pires, Maria Elisa [UNESP] Ferreira de Melo, Thais Regina [UNESP] Bosquesi, Priscila Longhin [UNESP] Chin, Chung Man [UNESP] Santos, Jean Leandro dos [UNESP] |
author2_role |
author author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (Unesp) |
dc.contributor.author.fl_str_mv |
Chelucci, Rafael Consolin [UNESP] Dutra, Luiz Antonio [UNESP] Lopes Pires, Maria Elisa [UNESP] Ferreira de Melo, Thais Regina [UNESP] Bosquesi, Priscila Longhin [UNESP] Chin, Chung Man [UNESP] Santos, Jean Leandro dos [UNESP] |
dc.subject.por.fl_str_mv |
hydrazone antiplatelet antithrombotic NSAIDs bleeding time |
topic |
hydrazone antiplatelet antithrombotic NSAIDs bleeding time |
description |
Nonsteroidal anti-inflammatory drugs (NSAIDs) 1-5 containing an N-acyl hydrazone subunit were prepared and their antiplatelet and antithrombotic activities assessed in vitro and in vivo. Compounds 1-5 inhibited the platelet aggregation induced by adenosine diphosphate and/or arachidonic acid, with inhibition rates of 18.0%-61.1% and 65.9%-87.3%, respectively. Compounds 1 and 5 were the most active compounds, inhibiting adenosine-diphosphate-induced platelet aggregation by 57.2% and 61.1%, respectively. The inhibitory rates for arachidonic-acid-induced platelet aggregation were similar for compound 2 (80.8%) and acetylsalicylic acid (ASA, 80%). After their oral administration to mice, compounds 1, 3, and 5 showed shorter mean bleeding times than ASA. Compounds 1 and 5 also protected against thromboembolic events, with survival rates of 40% and 33%, respectively, compared with 30% for ASA. In conclusion, these results indicate that these novel NSAIDs containing an NAH subunit may offer better antiplatelet and antithrombotic activities than ASA. |
publishDate |
2014 |
dc.date.none.fl_str_mv |
2014-12-03T13:11:43Z 2014-12-03T13:11:43Z 2014-02-01 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://dx.doi.org/10.3390/molecules19022089 Molecules. Basel: Mdpi Ag, v. 19, n. 2, p. 2089-2099, 2014. 1420-3049 http://hdl.handle.net/11449/113465 10.3390/molecules19022089 WOS:000334418200045 WOS000334418200045.pdf 9734333607975413 0000-0003-4141-0455 |
url |
http://dx.doi.org/10.3390/molecules19022089 http://hdl.handle.net/11449/113465 |
identifier_str_mv |
Molecules. Basel: Mdpi Ag, v. 19, n. 2, p. 2089-2099, 2014. 1420-3049 10.3390/molecules19022089 WOS:000334418200045 WOS000334418200045.pdf 9734333607975413 0000-0003-4141-0455 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Molecules 3.098 0,855 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
2089-2099 application/pdf |
dc.publisher.none.fl_str_mv |
Mdpi Ag |
publisher.none.fl_str_mv |
Mdpi Ag |
dc.source.none.fl_str_mv |
Web of Science reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
_version_ |
1808129455557705728 |