The anti-Alzheimer potential of some novel Tacrine-Coumarin Derivatives as a Cholinesterase inhibitor

Abstract

A series of Tacrine-coumarylthiazole derivatives linked through urea were synthesized, and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated for the treatment of Alzheimer's disease. The result revealed that all the synthesized compounds exhibited a moderate inhibitory effect on both cholinesterases. Amongst them, 1-(7-methoxy-1,2,3,4-tetrahydroacridin-9-yl)-3-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)urea (SC4, IC50= 37.09 µM) was found to be the most active compound against AChE, and 11-(6,8-dichloro-1,2,3,4-tetrahydroacridin-9-yl)-3-(4-(6-nitro-2-oxo-2H-chromen-3-yl)thiazol-2-yl)urea (SC10, IC50= 5.89 µM) exhibited the strongest inhibition against BuChE. The selectivity of SC4 and SC10 were 0.85 and 0.04, respectively.