6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents.
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.
Pavia
M R
MR
Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, Michigan 48105.
Taylor
C P
CP
Lobbestael
S J
SJ
D000631:Aminopyridines / Q000138:chemical synthesis / Q000627:therapeutic use* / Q000633:toxicity; D000818:Animals; D001259:Ataxia / Q000139:chemically induced; D001763:Blepharoptosis / Q000139:chemically induced; D055598:Chemical Phenomena; D002621:Chemistry; D004597:Electroshock; D007696:Kindling, Neurologic; D008297:Male; D051379:Mice; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D012640:Seizures / Q000188:drug therapy*; D013329:Structure-Activity Relationship
D000631:Aminopyridines