The syntheses of 4-acylaminopyridine derivatives and their high affini
ty choline uptake improvement activities are described. N-propylcarbon
yltetrahydroaminoacridine (1) was selected as a lead compound. Modific
ation of its ring structure and acyl moiety led some active compounds.
Among them, 9d (MKC-231) showed the highest activity. This compound i
s expected to be a unique medicine for Alzheimer's disease.