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

Insuasty, Henry Y Castro, Edison Y Escobar, Juan C. Y Murillo, Vanesa Y Rodríguez, Jeanette Y Cuca, Luis E, Y Estrada, Martín Y Insuasty, Braulio Y Guerrero, Mario F. (2014) Assessment of the anticonvulsant activity of pyrazolo[1,5-a][1,3,5]triazines obtained by synthesis. Revista Colombiana de Ciencias Químico-Farmacéuticas, 43 (1). pp. 22-38. ISSN 0034-7418

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Giving that the pyrazolo[1,5-a][1,3,5]triazine system is a potential source of phar-macological 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-/hetaroylimidodithiocarbon-ates and 5-aminopyrazoles were screened in vivo(300 mg/kg, v.o.) for their anticon-vulsant 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, 1 H and 13 C-NMR spectroscopic techniques, COSY 1 H-1 H, hsqcand hmbcexperiments, 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, picro-toxin, 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 Elemento: Artículo
Palabras Clave: pirazolotriazinas, anticonvulsivantes, evaluación preclínica de medi-camentos, electrochoque, relación estructura - actividad
Asunto: Q Ciencias > QD Chemistry
Division: Facultad de Ciencias Exactas y Naturales > Programa de Química > Productividad
Depósito de Usuario: doctor HENRY INSUASTY
Fecha Deposito: 31 Jan 2017 23:04
Ultima Modificación: 31 Jan 2017 23:04

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