Synthesis and anticonvulsant activity of some substituted lactams and amides

Journal of Medicinal Chemistry
1984.0

Abstract

Thirteen derivatives of 3-phenyl-2-piperidinone were synthesized and evaluated for anticonvulsant activity. The most active compounds from this group included two simple lactams, 3-hydroxy-1-methyl-3-phenyl-2-piperidinone and 3-methoxy-3-phenyl-2-piperidinone, and two N-ethoxycarbonyl lactams, 1-(ethoxycarbonyl)-3-hydroxy-3-phenyl-2-piperidinone and 1-(ethoxycarbonyl)-3-methoxy-3-phenyl-2-piperidinone, whose anticonvulsant activity was comparable to or better than that for valproic acid. Four related acyclic amides were also prepared, but these were essentially inactive as anticonvulsants.

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