Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 7, Pages 2101-2105Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.01.122
Keywords
Domino; Thiophenone; Malononitrile; Acetylcholinesterase; Alzheimer's disease
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Funding
- Department of Science and Technology, New Delhi
- DST-SERC Fast Track scheme [SR/FT/CS-073/2009]
- IRHPA program for the high resolution NMR facility in the Department
- University Grants Commission, New Delhi
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A library of novel 5-amino-2,7-diaryl-2,3-dihydrobenzo[b]thiophene-4,6-dicarbonitriles have been synthesized regioselectively in good yields through the one-pot domino reactions of 5-aryldihydro-3(2H)-thiophenones, malononitrile and aromatic aldehydes in the presence of morpholine. This transformation presumably involves Knoevenagel condensation-Michael addition-intramolecular Thorpe-Ziegler cyclization-Tautomerization-Elimination sequence of reactions. These compounds were evaluated for their acetylcholinesterase (AChE) inhibitory activity and 5-amino-2,7-bis(4-methoxyphenyl)-2,3-dihydrobenzo[b]thiophene-4,6-dicarbonitrile was found to be the most potent against AChE with IC50 4.16 mu mol/L. (C) 2013 Elsevier Ltd. All rights reserved.
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