Synthesis and biological evaluation of functionalized coumarins as acetylcholinesterase inhibitors

Three series of functionalized coumarin compounds were designed and prepared as cholinesterase (AChE and BuChE) inhibitors. The biological profile against AChE and BuChE of the prepared compounds was determined. Compound 7b exhibited a mixed-type of AChE inhibitor with IC50 value for the AChE inhibition of 0.19 ± 0.01 μM and a high selectivity for AChE/BuChE, and compound 6b acted as non-competitive AChE inhibitor with IC50 value of 0.43 ± 0.02 μM. Structure-activity relationships (SARs) of prepared compounds were discussed.