AMINOALKYLPYRIDINES 2- MOLECULAR MODIFICATION BY N-ACYLATION OF AMINOGROUP AND EFFECT ON ANTICONVULSANT ACTIVITY( )

Several N-acetylaminoalkylpyridines (N-acetylAAPs) (1a-4a) were synthe sized and tested for anticonvulsant activity in mice, ip, and rats, po . Several acetylating agents were investigated but excess acetic anhyd ride in refluxing benzene was the most effective. N-acetylation result ed in a decrease in the potent anticonvulsant activity of the parent A APs, particularly by the oral route, and at the same time, a considera ble increase in the neurotoxicity by the ip route.