Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021) - possible effects on phosphodiesterase

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dc.creatorMartins, Daniella Ramos
dc.creatorPazini, Francine
dc.creatorAlves, Vinícius de Medeiros
dc.creatorMoura, Soraya Santana de
dc.creatorLiao, Luciano Morais
dc.creatorMagalhães, Mariana Torquato Quezado de
dc.creatorValadares, Marize Campos
dc.creatorAndrade, Carolina Horta
dc.creatorMenegatti, Ricardo
dc.creatorRocha, Matheus Lavorenti
dc.date.accessioned2018-08-27T11:23:32Z
dc.date.available2018-08-27T11:23:32Z
dc.date.issued2013-05
dc.description.abstractThis 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 (45 mm), the treatment with tetraethylammonium (TEA) (5 mm) 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 toxicitypt_BR
dc.identifier.citationMARTINS, Daniella Ramos et al. Synthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021)-possible effects on phosphodiesterase. Chemical and Pharmaceutical Bulletin, Tokyo, v. 61, n. 5, p. 524-531, May 2013.pt_BR
dc.identifier.doi10.1248/cpb.c12-01016
dc.identifier.issn0009-2363
dc.identifier.issne- 1347-5223
dc.identifier.urihttp://repositorio.bc.ufg.br/handle/ri/15741
dc.language.isoengpt_BR
dc.publisher.countryBrasilpt_BR
dc.publisher.departmentInstituto de Química - IQ (RG)pt_BR
dc.rightsAcesso Abertopt_BR
dc.rights.uriAn error occurred getting the license - uri.*
dc.subjectPyrazolept_BR
dc.subjectPhosphodiesterasept_BR
dc.subjectRelaxationpt_BR
dc.subjectAortapt_BR
dc.subjectCyclic nucleotidept_BR
dc.titleSynthesis, docking studies, pharmacological activity and toxicity of a novel pyrazole derivative (LQFM 021) - possible effects on phosphodiesterasept_BR
dc.typeArtigopt_BR

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