Analgesic, Alzheimer's Disease/ACh Agonists: Novel 1-(Pyridinylamino)-2-Pyrrolidinones as Analgesics and Acetylcholine Agonists

Summary

Novelty: A novel series of substituted 1-(pyridinylamino)-2-pyrrolidinones are claimed as analgesics, memory enhancers and for the treatment of Alzheimer's disease.

Biology: Data are given for 1-(4-pyridmylamino)-2-pyrrolidinone in the phenylquinone-induced writhing assay in which 20 mg/kg sc showed 56% inhibition of writhing (aspirin ED₅₀ = 32.8 mg/kg sc). In the scopolamine dark avoidance assay, 1-(propyl-4-pyridinylamino)-2-pyrrolidinone oxalate shows a reversal in 33% of the animals with scopolamine induced-memory deficit at 0.3 mg/kg sc (tacrine showed 13% reversal at 0.63 mg/kg sc).

Chemistry: Two compounds are exemplified with a further seventeen named examples. These are prepared by arylation of a l-amino-2-pyrrolidinone with a halopyridine.