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 new mo...

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Main Author: Kia, Yalda
Format: Thesis
Language:English
Published: 2014
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Online Access:http://eprints.usm.my/46471/1/Yalda%20Kia24.pdf
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spelling my.usm.eprints.46471 http://eprints.usm.my/46471/ Synthesis, Characterization And Cholinesterase Inhibitory Activity Of Novel Piperidone Grafted Spiro Heterocycles Kia, Yalda 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 NonPeerReviewed application/pdf en http://eprints.usm.my/46471/1/Yalda%20Kia24.pdf Kia, Yalda (2014) Synthesis, Characterization And Cholinesterase Inhibitory Activity Of Novel Piperidone Grafted Spiro Heterocycles. PhD thesis, Universiti Sains Malaysia.
institution Universiti Sains Malaysia
building Hamzah Sendut Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Sains Malaysia
content_source USM Institutional Repository
url_provider http://eprints.usm.my/
language English
topic TP1-1185 Chemical technology
spellingShingle TP1-1185 Chemical technology
Kia, Yalda
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
author Kia, Yalda
author_facet Kia, Yalda
author_sort Kia, Yalda
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
publishDate 2014
url http://eprints.usm.my/46471/1/Yalda%20Kia24.pdf
http://eprints.usm.my/46471/
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score 13.211869