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Eur J Med Chem ; 41(6): 786-92, 2006 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-16647165

RESUMEN

A set of seven novel N-substituted 2-anilinophenylacetamides were designed by pharmacophore generation and using flexible alignment module of MOE software. The novel molecules were synthesized and screened for anticonvulsant activity in Swiss albino mice by MES and ScPTZ induced seizure tests. Test compounds were found to be potent in MES test. Compounds 12 and 14 were found to be more potent with ED(50) values 24.0 and 8.0 mg kg(-1), respectively, and their activity was comparable to standard drugs (Phenytoin, Carbamazepine). Test compounds did not show significant activity in ScPTZ test. Compounds 12 and 14 also exhibited higher protective indices (20.3 and 87.5, respectively) when assessed for neurotoxicity by rotarod test as compared to the standards.


Asunto(s)
Anticonvulsivantes/síntesis química , Anticonvulsivantes/farmacología , Fenilacetatos/síntesis química , Fenilacetatos/farmacología , Amidas/química , Animales , Anticonvulsivantes/química , Diseño de Fármacos , Ensayos de Selección de Medicamentos Antitumorales , Espectroscopía de Resonancia Magnética , Ratones , Modelos Moleculares , Fenilacetatos/química , Espectrofotometría Infrarroja
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