Title : Synthesis of aminoalkyl-substituted aurone derivatives as acetylcholinesterase inhibitors - Lee_2015_Bioorg.Med.Chem_23_231 |
Author(s) : Lee YH , Shin MC , Yun YD , Shin SY , Kim JM , Seo JM , Kim NJ , Ryu JH , Lee YS |
Ref : Bioorganic & Medicinal Chemistry , 23 :231 , 2015 |
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. |
PubMedSearch : Lee_2015_Bioorg.Med.Chem_23_231 |
PubMedID: 25468034 |
Lee YH, Shin MC, Yun YD, Shin SY, Kim JM, Seo JM, Kim NJ, Ryu JH, Lee YS (2015)
Synthesis of aminoalkyl-substituted aurone derivatives as acetylcholinesterase inhibitors
Bioorganic & Medicinal Chemistry
23 :231
Lee YH, Shin MC, Yun YD, Shin SY, Kim JM, Seo JM, Kim NJ, Ryu JH, Lee YS (2015)
Bioorganic & Medicinal Chemistry
23 :231