| Author | Martins, Daniella Ramos | |
| Author | Pazini, Francine | |
| Author | Alves, Vinícius de Medeiros | |
| Author | Moura, Soraya Santana de | |
| Author | Lião, Luciano Morais | |
| Author | Magalhães, Mariana Torquato Quezado de | |
| Author | Valadares, Marize Campos | |
| Author | Andrade, Carolina Horta | |
| Author | Menegatti, Ricardo | |
| Author | Rocha, Matheus Lavorenti | |
| Access date | 2019-10-01T14:53:19Z | |
| Available date | 2019-10-01T14:53:19Z | |
| Document date | 2013 | |
| Citation | 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. | pt_BR |
| ISSN | 0009-2363 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/36041 | |
| 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. | pt_BR |
| Language | eng | pt_BR |
| Publisher | Pharmaceutical Society of Japan | pt_BR |
| Rights | open access | pt_BR |
| Title | Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021): possible effects on phosphodiesterase | pt_BR |
| Type | Article | pt_BR |
| DOI | 10.1248/cpb.c12-01016 | |
| Abstract | 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. | pt_BR |
| Affilliation | Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil. | pt_BR |
| Affilliation | Federal University of Goias. Campus Samambaia. Chemistry Institute. Goiânia, GO, Brazil. | pt_BR |
| Affilliation | Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil. | pt_BR |
| Affilliation | Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil. | pt_BR |
| Affilliation | Federal University of Goias. Campus Samambaia. Chemistry Institute. Goiânia, GO, Brazil. | pt_BR |
| Affilliation | Embrapa Recursos Genéticos e Biotecnologia Brasília. Laboratory of Mass Spectrometry. Brasilia, DF, Brazil. | pt_BR |
| Affilliation | Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil. | pt_BR |
| Affilliation | Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil. | pt_BR |
| Affilliation | Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil. | pt_BR |
| Affilliation | Federal University of Goias. Faculty of Pharmacy. Goiânia, GO, Brazil. | pt_BR |
| Subject | Pyrazole | pt_BR |
| Subject | Phosphodiesterase | pt_BR |
| Subject | Relaxation | pt_BR |
| Subject | Aorta | pt_BR |
| Subject | Cyclic nucleotide | pt_BR |
| e-ISSN | 1347-5223 | |
