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Summary
Novelty: Novel ureas and thioureas are claimed to be acetylcholinesterase inhibitors. They may have utility in the treatment of Alzheimer's disease.
Biology: The acetylcholinesterase inhibitory activity was determined by the method of Ellman et al. (Biochem. Pharmacol. (1961) 7:88-95). Results for seven compounds are tabulated. IC50 values range between 1.5 and 260nM compared to tacrine which has a value of 120nM.
Chemistry: Synthesis was by standard techniques. Three compounds are exemplified by synthesis. Benzoyl-1-methyl-1-[2-(1-benzyl-piperidin-4-yl)ethylthiourea is an exemplified compound.
Structure: 