[Synthesis and AchE inhibitory activity of 2-phenoxy-indan-1-one derivatives].
OBJECTIVE
To design and synthesize novel AchE inhibitors.


METHODS
The condensation of 2-bromo-5, 6-dimethoxy-indan-1-one with various aminoalkyl phenols in the presence of K2CO3 and acetonitrile gave the corresponding title compounds, and the in vitro AchE and BchE inhibitory activities were evaluated by the modified Ellman method.


RESULTS
Sixteen novel target compounds 8a - p were synthesized, their structures were confirmed by 1H NMR, MS, IR and elemental analysis. Preliminary pharmacological test demonstrated that most of these compounds displayed high AchE inhibitory activities, the IC50 of the most potent inhibitor 8h was 50.0 nmol x L(-1), similar to that of Huperzine A (IC50 = 53.0 nmol x L(-1)), while all the compounds were almost inactive against BchE.


CONCLUSIONS
2-Phenoxy-indan-1-one derivatives exhibit high activities of AchE inhibition and are worthy of further investigation.
Sheng
Rong
R
ZJU-ENS Joint Laboratory of Medicinal Chemistry, School of Pharmaceutical Science, Zhejiang University, Hangzhou 310031, China.
Lin
Xiao
X
Li
Jing-ya
JY
Hu
Yong-zhou
YZ