ChemInform Abstract: Synthesis and Evaluation of Tacrine‐Related Compounds for the Treatment of Alzheimer′s Disease.

Abstract

Synthesis and Evaluation of Tacrine-Related Compounds for the Treatment of Alzheimer's Disease.-Friedlaender condensation of cyclic aminonitriles, e.g. (II), with dicarbonyl compounds such as (I), yields the products (IV)-(V). (IV) is a slightly less active inhibitor of acetylcholinesterase than tacrine with much lower toxicity. The structures of the educts (I) and (II) are largely varied as well as their ratio and the catalytic system to give products which have lower potency than (IV). -(AGUADO, F.; BADIA, A.; BANOS, J. E.; BOSCH, F.; BOZZO, C.; CAMPS, P.; CONTRERAS, J.; DIERSSEN, M.; ESCOLANO, C.; GOERBIG, D. M.; MUNOZ-TORRERO, D.; PUJOL, M. D.; SIMON, M.; VAZQUEZ, M. T.; VIVAS, N. M.; Eur.