JOURNAL 1399


Organic Communications
VOLUME & ISSUE
Available Online: November 04,2019
PAGES
p.1 - 8
DOI ADDRESS
http://doi.org/10.25135/acg.oc.69.19.09.1399
(DOI number will be activated after the manuscript has been available in an issue.)
STATISTICS
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AUTHORS
  • Sulunay Parlar
PDF OF ARTICLE

GRAPHICAL ABSTRACT


ABSTRACT


AA series of a,β-unsaturated carbonyl based piperidinone derivatives were synthesized and evaluated for their abilities to inhibit AChE and BuChE. All compounds exhibited AChE and BuChE inhibitory activity in different ratios. Among the series, compound 1d, (1-benzyl-3,5-bis(4-nitrobenzylidene)piperidine-4-one), was found to be the most potent derivative against AChE (IC50= 12.55 µM) and compound 1g, (1-benzyl-3,5-bis(4-chlorobenzylidene)piperidine-4-one) showed the best anti-BuChE activity (IC50= 17.28 µM). The derivatives exhibited selectivity on AChE enzyme with respect to BuChE. Only compound 1g, bearing chlorine substituents, demonstrated as a dual inhibitor of cholinesterases. Taken together, these results indicated that a,β-unsaturated carbonyl based piperidinone scaffold might be a promising drug candidate for further anti-AD drug development.

KEYWORDS
  • Acetylcholinesterase inhibitors
  • Butyrylcholinesterase inhibitors
  • Piperidinone
  • Alzheimer’s disease

SUPPORTING INFORMATION


Supporting Information
Download File 69-OC-1909-1399-SI.pdf (1.23 MB)