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Acta Pol Pharm ; 72(3): 489-96, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-26642657

RESUMEN

A series of potential anticonvulsants have been synthesized. There are eight fluorobenzylamides and three chlorobenzylamides of isocyclic or heterocyclic acids. Two not halogenated benzylamides were also synthesized to compare the effect of halogenation. The aim of the research performed was to evaluate whether halogenation of the mother structure is able to improve its anticonvulsant activity. The compounds were tested in Anticonvulsant Screening Project (ASP) of Antiepileptic Drug Development Program (ADDP) of NIH. Compound 1 showed MES ED50 = 80.32 mg/kg, PI = 3.16. Compound 7 showed CKM ED50 = 56.72 mg/kg. Compound 8 showed MES ED50 = 34.23 mg/kg and scPTZ ED50 > 300 mg/kg, PI = 8.53.Compound 13 showed 6Hz ED50 = 78.96, PI = 3.37. The results indicate that fluorination does not improve activity, whereas chlorination in our experiment even reduces it.


Asunto(s)
Ácidos Heterocíclicos/síntesis química , Amidas/síntesis química , Anticonvulsivantes/síntesis química , Compuestos de Bencilo/síntesis química , Ácidos Heterocíclicos/farmacología , Amidas/farmacología , Animales , Anticonvulsivantes/farmacología , Compuestos de Bencilo/farmacología , Ratones , Relación Estructura-Actividad
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