Synthesis and AchE inhibitory activity of 2-phenoxy-indan-1-one derivatives.
- Author:
Rong SHENG
1
;
Xiao LIN
;
Jing-ya LI
;
Yong-zhou HU
Author Information
- Publication Type:Journal Article
- MeSH: Acetylcholinesterase; metabolism; Animals; Cerebral Cortex; enzymology; Cholinesterase Inhibitors; chemical synthesis; chemistry; pharmacology; Drug Design; Indans; chemical synthesis; chemistry; pharmacology; Inhibitory Concentration 50; Molecular Structure; Rats; Structure-Activity Relationship
- From: Acta Pharmaceutica Sinica 2006;41(2):115-120
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo design and synthesize novel AchE inhibitors.
METHODSThe 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.
RESULTSSixteen 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.
CONCLUSION2-Phenoxy-indan-1-one derivatives exhibit high activities of AchE inhibition and are worthy of further investigation.
