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ID: ALA1149785
Journal: Eur J Med Chem
Title: Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors.
Authors: Wen H, Lin C, Que L, Ge H, Ma L, Cao R, Wan Y, Peng W, Wang Z, Song H.
Abstract: A series of helicid analogues were prepared and evaluated in vitro for the cholinesterase (AChE and BuChE) inhibitory activities via UV spectroscopy. The results indicated that compounds 5, 6d and 8 exhibited potent AChE inhibitory activities with IC(50) values of 0.45+/-0.02microM, 0.49+/-0.02microM, and 0.20+/-0.01microM, respectively. High selectivity for AChE over BuChE was also observed. Kinetic study showed that the mechanism of AChE inhibition of compounds 5, 6d and 8 was all mixed-type.
CiteXplore: 17574306