Synthesis, Characterization And Cholinesterase Inhibitory Activity Of Novel Piperidone Grafted Spiro Heterocycles

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 ne...

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Main Author: Yalda, Kia
Format: Thesis
Language:English
Published: 2014
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Online Access:http://eprints.usm.my/50165/1/Yalda%20Kia24.pdf
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spelling my-usm-ep.501652021-10-06T05:31:26Z Synthesis, Characterization And Cholinesterase Inhibitory Activity Of Novel Piperidone Grafted Spiro Heterocycles 2014-01 Yalda, Kia TP1-1185 Chemical technology 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. 2014-01 Thesis http://eprints.usm.my/50165/ http://eprints.usm.my/50165/1/Yalda%20Kia24.pdf application/pdf en public phd doctoral Universiti Sains Malaysia Pusat Pengajian Kejuruteraan Kimia
institution Universiti Sains Malaysia
collection USM Institutional Repository
language English
topic TP1-1185 Chemical technology
spellingShingle TP1-1185 Chemical technology
Yalda, Kia
Synthesis, Characterization And Cholinesterase Inhibitory Activity Of Novel Piperidone Grafted Spiro Heterocycles
description 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.
format Thesis
qualification_name Doctor of Philosophy (PhD.)
qualification_level Doctorate
author Yalda, Kia
author_facet Yalda, Kia
author_sort Yalda, Kia
title Synthesis, Characterization And Cholinesterase Inhibitory Activity Of Novel Piperidone Grafted Spiro Heterocycles
title_short Synthesis, Characterization And Cholinesterase Inhibitory Activity Of Novel Piperidone Grafted Spiro Heterocycles
title_full Synthesis, Characterization And Cholinesterase Inhibitory Activity Of Novel Piperidone Grafted Spiro Heterocycles
title_fullStr Synthesis, Characterization And Cholinesterase Inhibitory Activity Of Novel Piperidone Grafted Spiro Heterocycles
title_full_unstemmed Synthesis, Characterization And Cholinesterase Inhibitory Activity Of Novel Piperidone Grafted Spiro Heterocycles
title_sort synthesis, characterization and cholinesterase inhibitory activity of novel piperidone grafted spiro heterocycles
granting_institution Universiti Sains Malaysia
granting_department Pusat Pengajian Kejuruteraan Kimia
publishDate 2014
url http://eprints.usm.my/50165/1/Yalda%20Kia24.pdf
_version_ 1747822025109405696