Jeyachandran_2013_Bioorg.Med.Chem.Lett_23_2101

Reference

Title : A one-pot domino synthesis and discovery of highly functionalized dihydrobenzo[b]thiophenes as AChE inhibitors - Jeyachandran_2013_Bioorg.Med.Chem.Lett_23_2101
Author(s) : Jeyachandran V , Kumar RR , Ali MA , Choon TS
Ref : Bioorganic & Medicinal Chemistry Lett , 23 :2101 , 2013
Abstract :

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 mumol/L.

PubMedSearch : Jeyachandran_2013_Bioorg.Med.Chem.Lett_23_2101
PubMedID: 23434223

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Citations formats

Jeyachandran V, Kumar RR, Ali MA, Choon TS (2013)
A one-pot domino synthesis and discovery of highly functionalized dihydrobenzo[b]thiophenes as AChE inhibitors
Bioorganic & Medicinal Chemistry Lett 23 :2101

Jeyachandran V, Kumar RR, Ali MA, Choon TS (2013)
Bioorganic & Medicinal Chemistry Lett 23 :2101