부산대학교 도서관

A series of benzyl pyridinium-2,4-dioxochroman derivatives 7a-o were synthesized and evaluated as new agents for treatment of Alzheimer's disease. Among the synthesized compounds, compounds 7f and 7i exhibited the most potent anti-AChE and anti-BuChE activities, respectively. Kinetic study of compound 7f revealed that this compound inhibited AChE in a mixed-type inhibition mode. • A new series of benzyl pyridinium-2,4-dioxochromans 7a-o were synthesized as anti-Alzheimer agents. • Compounds 7f and 7i were the most potent AChE and BuChE inhibitors, respectively. • Compound 7f inhibited AChE by a mixed-type inhibition mode. • Docking study revealed that compound 7f binds to both the CS and PAS of AChE. A new series of benzyl pyridinium-2,4-dioxochroman derivatives 7a-o was synthesized and evaluated as new anti-Alzheimer agents. Among the synthesized compounds, the compounds 7f and 7i exhibited the most potent anti-AChE and anti-BuChE activities, respectively. The kinetic study of the compound 7f revealed that this compound inhibited AChE in a mixed-type inhibition mode. Furthermore, the docking study of the compounds 7f and 7i showed that these compounds bound to both the catalytic site (CS) and peripheral anionic site (PAS) of AChE and BuChE, respectively. The compound 7f also exhibited a greater self-induced Aβ peptide aggregation inhibitory activity in compare to donepezil. Furthermore, the neuroprotective activity of this compound at 20 μM was comparable to that of the standard neuroprotective agent (quercetin). [ABSTRACT FROM AUTHOR]