Zw. Lin et Pk. Kadaba, AMINOALKYLPYRIDINES 2- MOLECULAR MODIFICATION BY N-ACYLATION OF AMINOGROUP AND EFFECT ON ANTICONVULSANT ACTIVITY( ), Heterocyclic communications, 4(1), 1998, pp. 7-10
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.