Journal of Medicinal Chemistry p. 1210 - 1214 (1987)
Update date:2022-07-29
Topics:
Pavia, Michael R.
Taylor, Charles P.
Hershenson, Fred M.
Lobbestael, Sandra J.
The anticonvulsant effect of a series of 6-alkoxy-N,N-disubstituted-2-pyridinamines is described. An investigation was carried out to optimize the activity/side-effect ratio in this series of compounds. The most desirable profile was seen with 1-<6-(2-methylpropoxy)-2-pyridinyl>piperazine, 6, and this compound was selected for a more complete pharmacological evaluation. Overall, 6 has a pharmacological profile that is very similar to that of diphenylhydantoin (phenytoin). While nearly equipotent to phenytoin, animal studies suggest a fairly short duration of action. In addition, 6 exhibited some troublesome side effects including central nervous system depression and hypothermia.
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