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6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents
M R Pavia1, C P Taylor, S J Lobbestael
1Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, Michigan 48105.
Journal of Medicinal Chemistry
|June 1, 1989
Abstract:
The anticonvulsant effect of a series of 6-alkyl-N,N-disubstituted-2-pyridinamines is described. An investigation was carried out to optimize the anticonvulsant activity and reduce behavioral side effects in this series. Three compounds (7, 8, 10; Table I) were selected from initial screening for a more complete pharmacological evaluation. While each of these compounds was a potent anticonvulsant agent with ED50 values from 5 to 10 mg/kg, the activity was accompanied by significant behavioral side effects including decreased spontaneous locomotion, ataxia, and ptosis.