期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 10, 页码 2979-2983出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.03.027
关键词
AChE; BChE; 1,3-Dipolar cycloaddition; Selectivity and spiropyrrolizines
资金
- Malaysian Government
- Universiti Sains Malaysia [1001/PKIMIA/855006, 1001/PKIMIA/811221]
- University Sains Malaysia
A series of novel hybrid spiro heterocycles comprising pyrrolizine, spiroxindole and piperidine moieties was synthesized chemo-, regio- and stereoselectively in good yields from 1,3-dipolar cycloaddition reaction of a series of 1-acryloyl-3,5-bisarylmethylidenepiperidin-4-ones with azomethine ylides generated in situ from 5-choloroisatin and L-proline in methanol. These cycloadducts displayed significant cholinesterase inhibitory activity. Among the compounds screened, 8g and 8e, showed maximum inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinestrase (BChE) with IC50 values of 3.33 and 3.13 mu M, respectively. (C) 2013 Elsevier Ltd. All rights reserved.
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