title: Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors.
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.
authors.affiliation: School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China.
authors.forename: Huan
authors.initials: H
authors.lastname: Wen
authors.forename: Chonglan
authors.initials: C
authors.lastname: Lin
authors.forename: Ling
authors.initials: L
authors.lastname: Que
authors.forename: Hui
authors.initials: H
authors.lastname: Ge
authors.forename: Lin
authors.initials: L
authors.lastname: Ma
authors.forename: Rihui
authors.initials: R
authors.lastname: Cao
authors.forename: Yiqian
authors.initials: Y
authors.lastname: Wan
authors.forename: Wenlie
authors.initials: W
authors.lastname: Peng
authors.forename: Zihou
authors.initials: Z
authors.lastname: Wang
authors.forename: Huacan
authors.initials: H
authors.lastname: Song
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D001547:Benzaldehydes / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001688:Biological Products / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D006027:Glycosides / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D012545:Schiff Bases / Q000737:chemistry; D012680:Sensitivity and Specificity; D013056:Spectrophotometry, Ultraviolet
chemical_list: D001547:Benzaldehydes; D001688:Biological Products; D002800:Cholinesterase Inhibitors; D006027:Glycosides; D012545:Schiff Bases; C055677:helicide; D000110:Acetylcholinesterase