Synthesis of benzofuran derivatives via rearrangement and their inhibitory activity on acetylcholinesterase.
During a synthesis of coumarins to obtain new candidates for treating Alzheimer's Disease (AD), an unusual rearrangement of a benzopyran group to a benzofuran group occurred, offering a novel synthesis pathway of these benzofuran derivatives. The possible mechanism of the novel rearrangement was also discussed. All of the benzofuran derivatives have weak anti-AChE activities compared with the reference compound, donepezil.
Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China.
Xiang
X
Zhou
Miao
M
Li
Xiao-Bing
XB
Wang
Tao
T
Wang
Ling-Yi
LY
Kong
D000110:Acetylcholinesterase / Q000737:chemistry*; D000544:Alzheimer Disease / Q000188:drug therapy; D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis* / Q000737:chemistry*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry*; D058851:GPI-Linked Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry; D006801:Humans; D051381:Rats
D001572:Benzofurans; D002800:Cholinesterase Inhibitors; D058851:GPI-Linked Proteins; D000110:Acetylcholinesterase; C548246:Ache protein, rat