Synthesis and acetylcholinesterase inhibition of derivatives of huperzine B.
By targeting dual active sites of AChE, a number of new derivatives of HupB have been synthesized and tested as acetylcholinesterase inhibitors. The most potent compound, bis-HupB 5b is 72-fold more potent in AChE inhibition and 79-fold more selective for AChE versus BChE than HupB.
Feng
Song
S
State Key Laboratory for New Drug Research, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China.
Xia
Yu
Y
Han
Dongmei
D
Zheng
Chunyan
C
He
Xuchang
X
Tang
Xican
X
Bai
Donglu
D
D000470:Alkaloids / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001665:Binding Sites; D002540:Cerebral Cortex; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D004365:Drugs, Chinese Herbal / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
D000470:Alkaloids; D002800:Cholinesterase Inhibitors; D004365:Drugs, Chinese Herbal; C053016:huperzine B