Synthesis and biological evaluation of functionalized coumarins as acetylcholinesterase inhibitors.
Three series of functionalized coumarin compounds were designed and prepared as cholinesterase (AChE and BuChE) inhibitors. The biological profile against AChE and BuChE of the prepared compounds was determined. Compound 7b exhibited a mixed-type of AChE inhibitor with IC50 value for the AChE inhibition of 0.19+/-0.01 microM and a high selectivity for AChE/BuChE, and compound 6b acted as non-competitive AChE inhibitor with IC50 value of 0.43+/-0.02 microM. Structure-activity relationships (SARs) of prepared compounds were discussed.
Shen
Qiong
Q
School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275, China.
Peng
Quan
Q
Shao
Jialiang
J
Liu
Xufeng
X
Huang
Zhishu
Z
Pu
Xianzhang
X
Ma
Lin
L
Li
Yue-Ming
YM
Chan
Albert S C
AS
Gu
Lianquan
L
D000110:Acetylcholinesterase / Q000737:chemistry / Q000187:drug effects*; D002091:Butyrylcholinesterase / Q000737:chemistry / Q000187:drug effects; D002384:Catalysis; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D006868:Hydrolysis; D007700:Kinetics; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D002800:Cholinesterase Inhibitors; D003374:Coumarins; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase