Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021): possible effects on phosphodiesterase
| Autor(a) principal: | |
|---|---|
| Data de Publicação: | 2013 |
| Outros Autores: | , , , , , , , , |
| Tipo de documento: | Artigo |
| Idioma: | eng |
| Título da fonte: | Repositório Institucional da FIOCRUZ (ARCA) |
| Texto Completo: | https://www.arca.fiocruz.br/handle/icict/36041 |
Resumo: | Soraya Santana de Moura. Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Documento produzido em parceria ou por autor vinculado à Fiocruz, mas não consta a informação no documento. |
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Martins, Daniella RamosPazini, FrancineAlves, Vinícius de MedeirosMoura, Soraya Santana deLião, Luciano MoraisMagalhães, Mariana Torquato Quezado deValadares, Marize CamposAndrade, Carolina HortaMenegatti, RicardoRocha, Matheus Lavorenti2019-10-01T14:53:19Z2019-10-01T14:53:19Z2013MOURA, Soraya Santana de et al. Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021)--possible effects on phosphodiesterase. Chemical and Pharmaceutical Bulletin, v. 61, n. 5, p. 524-531, 2013.0009-2363https://www.arca.fiocruz.br/handle/icict/3604110.1248/cpb.c12-010161347-5223Soraya Santana de Moura. Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Documento produzido em parceria ou por autor vinculado à Fiocruz, mas não consta a informação no documento.Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil.Federal University of Goias. Campus Samambaia. Chemistry Institute. Goiânia, GO, Brazil.Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil.Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil.Federal University of Goias. Campus Samambaia. Chemistry Institute. Goiânia, GO, Brazil.Embrapa Recursos Genéticos e Biotecnologia Brasília. Laboratory of Mass Spectrometry. Brasilia, DF, Brazil.Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil.Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil.Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil.Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil.This study describes the synthetic route and molecular computational docking of LQFM 021, as well as examines its biological effects and toxicity. The docking studies revealed strong interaction of LQFM 021 to phosphodiesterase-3 (PDE-3). In isolated arteries, the presence of endothelium potentiates the relaxation for LQFM 021 and the inhibition cyclic nucleotides reduced the relaxation. Pre-contraction with KCl (45mm), the treatment with tetraethylammonium (TEA) (5mm) and inhibition of reticular Ca2+-ATPase showed an inhibitory effect on relaxation. Moreover, the compound reduced the contraction evoked by the Ca2+ influx. Acute toxicity tests revealed that the compound was practically nontoxic. In conclusion, this study showed that a new synthetic derivative of pyrazole is a possible PDE-3 inhibitor and has vasorelaxant activity and low toxicity.engPharmaceutical Society of JapanSynthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021): possible effects on phosphodiesteraseinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlePyrazolePhosphodiesteraseRelaxationAortaCyclic nucleotideinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txttext/plain1748https://www.arca.fiocruz.br/bitstream/icict/36041/1/license.txt8a4605be74aa9ea9d79846c1fba20a33MD51ORIGINALve_Martins_Daniella_etal_INI_2013.pdfve_Martins_Daniella_etal_INI_2013.pdfapplication/pdf1665526https://www.arca.fiocruz.br/bitstream/icict/36041/2/ve_Martins_Daniella_etal_INI_2013.pdf189fbbdf2a23de5824a0873a8a5f4bf3MD52TEXTve_Martins_Daniella_etal_INI_2013.pdf.txtve_Martins_Daniella_etal_INI_2013.pdf.txtExtracted texttext/plain40735https://www.arca.fiocruz.br/bitstream/icict/36041/3/ve_Martins_Daniella_etal_INI_2013.pdf.txt6312da0b05f3652d2b4c47ed4585aa2eMD53icict/360412019-10-06 12:29:01.893oai:www.arca.fiocruz.br:icict/36041Tk9URTogUExBQ0UgWU9VUiBPV04gTElDRU5TRSBIRVJFClRoaXMgc2FtcGxlIGxpY2Vuc2UgaXMgcHJvdmlkZWQgZm9yIGluZm9ybWF0aW9uYWwgcHVycG9zZXMgb25seS4KCk5PTi1FWENMVVNJVkUgRElTVFJJQlVUSU9OIExJQ0VOU0UKCkJ5IHNpZ25pbmcgYW5kIHN1Ym1pdHRpbmcgdGhpcyBsaWNlbnNlLCB5b3UgKHRoZSBhdXRob3Iocykgb3IgY29weXJpZ2h0Cm93bmVyKSBncmFudHMgdG8gRFNwYWNlIFVuaXZlcnNpdHkgKERTVSkgdGhlIG5vbi1leGNsdXNpdmUgcmlnaHQgdG8gcmVwcm9kdWNlLAp0cmFuc2xhdGUgKGFzIGRlZmluZWQgYmVsb3cpLCBhbmQvb3IgZGlzdHJpYnV0ZSB5b3VyIHN1Ym1pc3Npb24gKGluY2x1ZGluZwp0aGUgYWJzdHJhY3QpIHdvcmxkd2lkZSBpbiBwcmludCBhbmQgZWxlY3Ryb25pYyBmb3JtYXQgYW5kIGluIGFueSBtZWRpdW0sCmluY2x1ZGluZyBidXQgbm90IGxpbWl0ZWQgdG8gYXVkaW8gb3IgdmlkZW8uCgpZb3UgYWdyZWUgdGhhdCBEU1UgbWF5LCB3aXRob3V0IGNoYW5naW5nIHRoZSBjb250ZW50LCB0cmFuc2xhdGUgdGhlCnN1Ym1pc3Npb24gdG8gYW55IG1lZGl1bSBvciBmb3JtYXQgZm9yIHRoZSBwdXJwb3NlIG9mIHByZXNlcnZhdGlvbi4KCllvdSBhbHNvIGFncmVlIHRoYXQgRFNVIG1heSBrZWVwIG1vcmUgdGhhbiBvbmUgY29weSBvZiB0aGlzIHN1Ym1pc3Npb24gZm9yCnB1cnBvc2VzIG9mIHNlY3VyaXR5LCBiYWNrLXVwIGFuZCBwcmVzZXJ2YXRpb24uCgpZb3UgcmVwcmVzZW50IHRoYXQgdGhlIHN1Ym1pc3Npb24gaXMgeW91ciBvcmlnaW5hbCB3b3JrLCBhbmQgdGhhdCB5b3UgaGF2ZQp0aGUgcmlnaHQgdG8gZ3JhbnQgdGhlIHJpZ2h0cyBjb250YWluZWQgaW4gdGhpcyBsaWNlbnNlLiBZb3UgYWxzbyByZXByZXNlbnQKdGhhdCB5b3VyIHN1Ym1pc3Npb24gZG9lcyBub3QsIHRvIHRoZSBiZXN0IG9mIHlvdXIga25vd2xlZGdlLCBpbmZyaW5nZSB1cG9uCmFueW9uZSdzIGNvcHlyaWdodC4KCklmIHRoZSBzdWJtaXNzaW9uIGNvbnRhaW5zIG1hdGVyaWFsIGZvciB3aGljaCB5b3UgZG8gbm90IGhvbGQgY29weXJpZ2h0LAp5b3UgcmVwcmVzZW50IHRoYXQgeW91IGhhdmUgb2J0YWluZWQgdGhlIHVucmVzdHJpY3RlZCBwZXJtaXNzaW9uIG9mIHRoZQpjb3B5cmlnaHQgb3duZXIgdG8gZ3JhbnQgRFNVIHRoZSByaWdodHMgcmVxdWlyZWQgYnkgdGhpcyBsaWNlbnNlLCBhbmQgdGhhdApzdWNoIHRoaXJkLXBhcnR5IG93bmVkIG1hdGVyaWFsIGlzIGNsZWFybHkgaWRlbnRpZmllZCBhbmQgYWNrbm93bGVkZ2VkCndpdGhpbiB0aGUgdGV4dCBvciBjb250ZW50IG9mIHRoZSBzdWJtaXNzaW9uLgoKSUYgVEhFIFNVQk1JU1NJT04gSVMgQkFTRUQgVVBPTiBXT1JLIFRIQVQgSEFTIEJFRU4gU1BPTlNPUkVEIE9SIFNVUFBPUlRFRApCWSBBTiBBR0VOQ1kgT1IgT1JHQU5JWkFUSU9OIE9USEVSIFRIQU4gRFNVLCBZT1UgUkVQUkVTRU5UIFRIQVQgWU9VIEhBVkUKRlVMRklMTEVEIEFOWSBSSUdIVCBPRiBSRVZJRVcgT1IgT1RIRVIgT0JMSUdBVElPTlMgUkVRVUlSRUQgQlkgU1VDSApDT05UUkFDVCBPUiBBR1JFRU1FTlQuCgpEU1Ugd2lsbCBjbGVhcmx5IGlkZW50aWZ5IHlvdXIgbmFtZShzKSBhcyB0aGUgYXV0aG9yKHMpIG9yIG93bmVyKHMpIG9mIHRoZQpzdWJtaXNzaW9uLCBhbmQgd2lsbCBub3QgbWFrZSBhbnkgYWx0ZXJhdGlvbiwgb3RoZXIgdGhhbiBhcyBhbGxvd2VkIGJ5IHRoaXMKbGljZW5zZSwgdG8geW91ciBzdWJtaXNzaW9uLgo=Repositório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352019-10-06T15:29:01Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false |
| dc.title.pt_BR.fl_str_mv |
Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021): possible effects on phosphodiesterase |
| title |
Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021): possible effects on phosphodiesterase |
| spellingShingle |
Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021): possible effects on phosphodiesterase Martins, Daniella Ramos Pyrazole Phosphodiesterase Relaxation Aorta Cyclic nucleotide |
| title_short |
Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021): possible effects on phosphodiesterase |
| title_full |
Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021): possible effects on phosphodiesterase |
| title_fullStr |
Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021): possible effects on phosphodiesterase |
| title_full_unstemmed |
Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021): possible effects on phosphodiesterase |
| title_sort |
Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021): possible effects on phosphodiesterase |
| author |
Martins, Daniella Ramos |
| author_facet |
Martins, Daniella Ramos Pazini, Francine Alves, Vinícius de Medeiros Moura, Soraya Santana de Lião, Luciano Morais Magalhães, Mariana Torquato Quezado de Valadares, Marize Campos Andrade, Carolina Horta Menegatti, Ricardo Rocha, Matheus Lavorenti |
| author_role |
author |
| author2 |
Pazini, Francine Alves, Vinícius de Medeiros Moura, Soraya Santana de Lião, Luciano Morais Magalhães, Mariana Torquato Quezado de Valadares, Marize Campos Andrade, Carolina Horta Menegatti, Ricardo Rocha, Matheus Lavorenti |
| author2_role |
author author author author author author author author author |
| dc.contributor.author.fl_str_mv |
Martins, Daniella Ramos Pazini, Francine Alves, Vinícius de Medeiros Moura, Soraya Santana de Lião, Luciano Morais Magalhães, Mariana Torquato Quezado de Valadares, Marize Campos Andrade, Carolina Horta Menegatti, Ricardo Rocha, Matheus Lavorenti |
| dc.subject.en.pt_BR.fl_str_mv |
Pyrazole Phosphodiesterase Relaxation Aorta Cyclic nucleotide |
| topic |
Pyrazole Phosphodiesterase Relaxation Aorta Cyclic nucleotide |
| description |
Soraya Santana de Moura. Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Documento produzido em parceria ou por autor vinculado à Fiocruz, mas não consta a informação no documento. |
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2013 |
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2013 |
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2019-10-01T14:53:19Z |
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2019-10-01T14:53:19Z |
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info:eu-repo/semantics/publishedVersion |
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info:eu-repo/semantics/article |
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MOURA, Soraya Santana de et al. Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021)--possible effects on phosphodiesterase. Chemical and Pharmaceutical Bulletin, v. 61, n. 5, p. 524-531, 2013. |
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https://www.arca.fiocruz.br/handle/icict/36041 |
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0009-2363 |
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10.1248/cpb.c12-01016 |
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1347-5223 |
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MOURA, Soraya Santana de et al. Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021)--possible effects on phosphodiesterase. Chemical and Pharmaceutical Bulletin, v. 61, n. 5, p. 524-531, 2013. 0009-2363 10.1248/cpb.c12-01016 1347-5223 |
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Pharmaceutical Society of Japan |
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Pharmaceutical Society of Japan |
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