Synthesis and pharmacological evaluation of a major metabolite of ameltolide, a potent anticonvulsant

DW Robertson, EE Beedle, JH Krushinski…

文献索引：Robertson; Beedle; Krushinski; Lawson; Parli; Potts; Leander Journal of Medicinal Chemistry, 1991 , vol. 34, # 4 p. 1253 - 1257

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被引用次数: 6

摘要

This metabolite was prepared in five steps from a readily available starting material. Compound 7 and its nonacetylated analogue 6 were compared to ameltolide as anticonvulsants. After oral administration to mice, the MES EDSo values of ameltolide, 6, and 7 were 1.4, 10.9, and> lo0 mg/kg, respectively, demonstrating that hydroxylation and acetylation dramatically decrease the anticonvulsant potency of ameltolide. This rank ...