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Assessment of the anticonvulsant activity of pyrazolo[1,5-a][1,3,5]triazines obtained by synthesis

Insuasty, Henry and Castro, Edinson and Escobar, Juan C and Murillo, Vanesa and Rodriguez, Jeanette and Cuca, Luis and Estrada, Martin and Insuasty, Braulio and Guerrero, Mario (2014) Assessment of the anticonvulsant activity of pyrazolo[1,5-a][1,3,5]triazines obtained by synthesis. Revista Colombiana de Ciencias Químico Farmacéuticas; Vol. 43, núm. 1 (2014); 22-38 0034-7418 1909-6356 .

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Resumen

Giving that the pyrazolo[1,5-a][1,3,5]triazine system is a potential source of pharmacological agents for treatment of central nervous system disorders this work was aimed to asses anticonvulsant and acute neurotoxic effects of six molecules obtained by synthesis, using experimental models in mice. A series of six pyrazolo[1,5-a] [1,3,5]triazines (EAC-21, EAC-31, EAC-33, MH4a, MH4b1 and MH4c) obtained by one-step reaction from S,S-diethyl aroyl-/hetaroylimidodithiocarbonates and 5-aminopyrazoles were screened in vivo (300 mg/kg, v.o.) for their anticonvulsant activity in the maximal electroshock (MES) test in ICR mice and for acute toxicity in the rota-rod and wiring test. The structures of the obtained compounds were unambiguously established by IR, 1H and 13C-NMR spectroscopic techniques, COSY 1H-1H, hsqc and hmbc experiments, mass spectrometry and elemental analyses. Results shown that only MH4b1 showed protection against MES (p < 0.05) and was devoid of gross neurotoxicity signs. Therefore, MH4b1 was chosen for additional anticonvulsant screening against MES, pentylenetetrazole, picrotoxin, strychnine and 6 Hz psychomotor seizure model, in a dose dependent manner (50, 150, 300 mg/kg, v.o.). MH4b1 also protected against 6 Hz seizure test (> 150 mg/kg, v.o.). These data suggest that MH4b1 could be a source for anticonvulsant pyrazolo[1,5-a][1,3,5]triazine analogs potentially useful against tonic clonic and refractory seizures.

Tipo de documento:Artículo - Article
Información adicional:Departamento de Farmacia-Facultad de Ciencias Universidad Nacional de Colombia Se autoriza la fotocopia de articulos y textos para fines de uso académico o interno de las instituciones citando la fuente. Las ideas emitidas por los autores son reponsabilidad expresa de estos y no de la revista.
Palabras clave:pyrazolotriazines, anticonvulsants, drug screening, electroshock, structure- activity relationship.
Unidad administrativa:Revistas electrónicas UN > Revista Colombiana de Ciencias Químico Farmacéuticas
Código ID:42880
Enviado por : Dirección Nacional de Bibliotecas STECNICO
Enviado el día :13 Septiembre 2014 10:10
Ultima modificación:13 Septiembre 2014 10:10
Ultima modificación:13 Septiembre 2014 10:10
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