Synthesis and anticholinesterase activity of huperzine A analogues containing phenol and catechol replacements for the pyridone ring

G Campiani, AP Kozikowski, S Wang, L Ming…

文献索引：Campiani, Giuseppe; Kozikowski, Alan P.; Wang, Shaomeng; Ming, Liu; Nacci, Vito; Saxena, Ashima; Doctor, Bhupendra P. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 11 p. 1413 - 1418

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被引用次数: 32

摘要

Based upon modeling results obtained using the crystal structure of huperzine A in complex with acetylcholinesterase (AChE), two novel analogues of this potent AChE inhibitor were designed with phenol or catechol rings replacing the pyridone ring. From the modeling studies, the catechol analogue appeared capable of replacing one of the crystallographic waters bridging huperzine with Tyr 130 and Glu 199 of AChE. The synthesis of these ...