Lee_2015_Bioorg.Med.Chem_23_231

Reference

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

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Citations formats

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