Yalda, Kia
(2014)
Synthesis, Characterization And
Cholinesterase Inhibitory Activity Of
Novel Piperidone Grafted Spiro
Heterocycles.
PhD thesis, Universiti Sains Malaysia.
Abstract
Five new series of new spiro-oxindole-pyrrolizine and pyrrolidine hybrids were
synthesized employing facile one-pot three-component reaction of linear or cyclic
α-amino acids, isatin and various derivatives of N-acryloyl-bis arylidene piperidin-4-
ones dipolarophiles.
These reactions afforded new mono-spiroheterocycles and bis-spiroheterocycles by
changing the ratio of the starting materials from 1:1:1 to 1:2:2 of dipolarophiles,
α-amino acid and isatin. These spiro-cycloadducts were further elucidated using
elemental analysis, IR, 1-D and 2-D NMR spectroscopy techniques as well as X-Ray
crystallographic data.
The newly synthesized compounds were also evaluated for their activity against
Alzheimer’s disease using Ellman’s colorimetric assay. In this assay the cholinesterase
inhibitory activity of the aforementioned compounds were screened in vitro against
acetylcholinesterase enzyme (AChE) from electric eel and butyrylcholinesterase enzyme
(BChE) from equine serum, which have the major roles in the manifestation and
progression of Alzheimer’s disease.
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