title: Synthesis of aminoalkyl-substituted aurone derivatives as acetylcholinesterase inhibitors.
abstract: Alzheimer's disease (AD), a progressive and neurodegenerative disorder of the brain, is the most common cause of dementia among elderly people. To date, the successful therapeutic strategy to treat AD is maintaining the levels of acetylcholine by inhibiting acetylcholinesterase (AChE). In the present study, aurone derivatives were designed and synthesized as AChE inhibitors based on the lead structure of sulfuretin. Of those synthesized, compound 10d showed ca. 1700-fold and 6-fold higher AChE inhibitory activity than sulfuretin and galantamine, respectively. This compound also ameliorated scopolamine-induced memory deficit in mice when administered orally at the dose of 1 and 2mg/kg.
authors.affiliation: Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea; Medicinal Chemistry Laboratory, Department of Pharmacy, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea.
authors.forename: Young Hun
authors.initials: YH
authors.lastname: Lee
authors.affiliation: Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea; Medicinal Chemistry Laboratory, Department of Pharmacy, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea.
authors.forename: Min Cheol
authors.initials: MC
authors.lastname: Shin
authors.affiliation: Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea; Medicinal Chemistry Laboratory, Department of Pharmacy, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea.
authors.forename: Yong Don
authors.initials: YD
authors.lastname: Yun
authors.affiliation: Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea; Medicinal Chemistry Laboratory, Department of Pharmacy, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea.
authors.forename: Seo Young
authors.initials: SY
authors.lastname: Shin
authors.affiliation: Department of Oriental Pharmaceutical Science, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea.
authors.forename: Jong Min
authors.initials: JM
authors.lastname: Kim
authors.affiliation: Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea; Medicinal Chemistry Laboratory, Department of Pharmacy, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea.
authors.forename: Jeong Moo
authors.initials: JM
authors.lastname: Seo
authors.affiliation: Medicinal Chemistry Laboratory, Department of Pharmacy, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea.
authors.forename: Nam-Jung
authors.initials: NJ
authors.lastname: Kim
authors.affiliation: Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea; Department of Oriental Pharmaceutical Science, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea.
authors.forename: Jong Hoon
authors.initials: JH
authors.lastname: Ryu
authors.affiliation: Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea; Medicinal Chemistry Laboratory, Department of Pharmacy, College of Pharmacy, Kyung Hee University, 26 Kyungheedae-ro, Seoul 130-701, Republic of Korea. Electronic address: kyslee@khu.ac.kr.
authors.forename: Yong Sup
authors.initials: YS
authors.lastname: Lee
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy; D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D051379:Mice
chemical_list: D001572:Benzofurans; D002800:Cholinesterase Inhibitors; C486837:aurone
keywords: Acetylcholinesterase inhibitor; Alzheimer’s disease; Aurone; Galantamine; Memory enhancing; Sulfuretin