3-Phenoxypyridine 1-oxides as anticonvulsant agents.

Pavia, M R; Taylor, C P; Hershenson, F M; Lobbestael, S J; Butler, D E

Pavia, M R; Taylor, C P; Hershenson, F M; Lobbestael, S J; Butler, D E.

Afiliación

Pavia MR; Department of Chemistry, Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, Michigan 48104.

J Med Chem ; 31(4): 841-7, 1988 Apr.

Article en En | MEDLINE | ID: mdl-3351862

RESUMEN

The anticonvulsant activity of a series of 3-phenoxypyridine 1-oxides is described. An investigation carried out to optimize the activity/side effect ratio provided 4-methyl-3-phenoxypyridine 1-oxide, 3, as the derivative of choice. Overall, 3 has a pharmacological profile that is very similar to phenytoin. It exhibited significant anticonvulsant activity at doses that did not produce ataxia or sedation but caused increased spontaneous behavioral activity not seen with most anticonvulsants. The short duration of pharmacological effect of 3 was attributed to metabolic hydroxylation at the C-4 pyridine methyl group; however, structural modifications designed to inhibit this metabolic pathway were unsuccessful.

Asunto(s)

Anticonvulsivantes/síntesis química; Óxidos N-Cíclicos/síntesis química; Piridinas/síntesis química; Animales; Anticonvulsivantes/farmacología; Condicionamiento Operante/efectos de los fármacos; Óxidos N-Cíclicos/farmacología; Hidroxilación; Masculino; Ratones; Actividad Motora/efectos de los fármacos; Piridinas/farmacología; Relación Estructura-Actividad; Factores de Tiempo

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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piridinas / Óxidos N-Cíclicos / Anticonvulsivantes Límite: Animals Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 1988 Tipo del documento: Article Pais de publicación: Estados Unidos

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