Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 24, Issue 6, Pages 1408-1417Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2016.02.019
Keywords
Spiro-dihydropyridines; Multi-component reactions; Catalyst-free; Acetylcholinesterase inhibition; Butyrylcholinesterase inhibition
Funding
- Persian Gulf University Research Councils
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A simple, efficient and green approach for the synthesis of spiro-dihydropyridines derivatives by one -pot multi -component reaction of isatin or acenaphthoquinone derivatives (1 equiv) with malononitrile (1 equiv) and N,N'-substituted-2-nitroethene-1,1-diamines (1 equiv) in PEG -400 under catalyst-free conditions is described. This method provides several advantages such as environmental friendliness, short reaction time, and simple workup procedure for the synthesis of biologically important compounds. The ability of synthesized compounds in inhibition of acetyl and butyrylcholinesterase were investigated both in vitro and in silico. All compounds showed moderate to high level activity against both acetyl and butyrylcholinesterase. There was a good correlation between in vitro and in silico studies. (C) 2016 Elsevier Ltd. All rights reserved.
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