Synthesis, Cholinesterase Inhibitory Activity And Molecular Docking Study Of Piperidone-Grafted Pyrimidine And Thiazolopyrimidine Derivatives

Alzheimer’s disease (AD) is the most common form of dementia among the elderly people. Based on the cholinergic hypothesis, loss of cholinergic neurons in AD patients’ brain leads to the decline of acetylcholine (ACh) neurotransmitter level and eventually causes severe dysfunctions in the cholinergi...

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Main Author:	Basiri, Alireza
Format:	Thesis
Language:	English
Published:	2014
Subjects:	RS1-441 Pharmacy and materia medica
Online Access:	http://eprints.usm.my/46371/1/Alireza%20Basiri24.pdf
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id	my-usm-ep.46371
record_format	uketd_dc
spelling	my-usm-ep.463712020-02-27T08:38:31Z Synthesis, Cholinesterase Inhibitory Activity And Molecular Docking Study Of Piperidone-Grafted Pyrimidine And Thiazolopyrimidine Derivatives 2014-01 Basiri, Alireza RS1-441 Pharmacy and materia medica Alzheimer’s disease (AD) is the most common form of dementia among the elderly people. Based on the cholinergic hypothesis, loss of cholinergic neurons in AD patients’ brain leads to the decline of acetylcholine (ACh) neurotransmitter level and eventually causes severe dysfunctions in the cholinergic neurotransmission. Thus, increasing the ACh levels is a promising therapeutic approach to restore the substantial impairment of memory and cognitive dysfunctions in AD patients. The search for new cholinesterase inhibitors is still ongoing worldwide. Inspired by the biological significance of pyrimidine-grafted derivatives, especially in cholinesterase inhibition, seventy-four novel pyrimidine embedded derivatives, namely pyridopyrimidines 6(a-l), pyridopyrimidothiones 7(a-l), N-ethyl-pyridopyrimidothiones 8(a-j), N-ethylmorpholino pyridopyrimidothiones 9(a-j), pyrimidinethiols 11(a-l) and thiazolopyrimidines 13(a-r) were synthesized and evaluated for their cholinesterases inhibitory potential against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). 2014-01 Thesis http://eprints.usm.my/46371/ http://eprints.usm.my/46371/1/Alireza%20Basiri24.pdf application/pdf en public phd doctoral Universiti Sains Malaysia Pusat Pengajian Sains Farmasi
institution	Universiti Sains Malaysia
collection	USM Institutional Repository
language	English
topic	RS1-441 Pharmacy and materia medica
spellingShingle	RS1-441 Pharmacy and materia medica Basiri, Alireza Synthesis, Cholinesterase Inhibitory Activity And Molecular Docking Study Of Piperidone-Grafted Pyrimidine And Thiazolopyrimidine Derivatives
description	Alzheimer’s disease (AD) is the most common form of dementia among the elderly people. Based on the cholinergic hypothesis, loss of cholinergic neurons in AD patients’ brain leads to the decline of acetylcholine (ACh) neurotransmitter level and eventually causes severe dysfunctions in the cholinergic neurotransmission. Thus, increasing the ACh levels is a promising therapeutic approach to restore the substantial impairment of memory and cognitive dysfunctions in AD patients. The search for new cholinesterase inhibitors is still ongoing worldwide. Inspired by the biological significance of pyrimidine-grafted derivatives, especially in cholinesterase inhibition, seventy-four novel pyrimidine embedded derivatives, namely pyridopyrimidines 6(a-l), pyridopyrimidothiones 7(a-l), N-ethyl-pyridopyrimidothiones 8(a-j), N-ethylmorpholino pyridopyrimidothiones 9(a-j), pyrimidinethiols 11(a-l) and thiazolopyrimidines 13(a-r) were synthesized and evaluated for their cholinesterases inhibitory potential against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE).
format	Thesis
qualification_name	Doctor of Philosophy (PhD.)
qualification_level	Doctorate
author	Basiri, Alireza
author_facet	Basiri, Alireza
author_sort	Basiri, Alireza
title	Synthesis, Cholinesterase Inhibitory Activity And Molecular Docking Study Of Piperidone-Grafted Pyrimidine And Thiazolopyrimidine Derivatives
title_short	Synthesis, Cholinesterase Inhibitory Activity And Molecular Docking Study Of Piperidone-Grafted Pyrimidine And Thiazolopyrimidine Derivatives
title_full	Synthesis, Cholinesterase Inhibitory Activity And Molecular Docking Study Of Piperidone-Grafted Pyrimidine And Thiazolopyrimidine Derivatives
title_fullStr	Synthesis, Cholinesterase Inhibitory Activity And Molecular Docking Study Of Piperidone-Grafted Pyrimidine And Thiazolopyrimidine Derivatives
title_full_unstemmed	Synthesis, Cholinesterase Inhibitory Activity And Molecular Docking Study Of Piperidone-Grafted Pyrimidine And Thiazolopyrimidine Derivatives
title_sort	synthesis, cholinesterase inhibitory activity and molecular docking study of piperidone-grafted pyrimidine and thiazolopyrimidine derivatives
granting_institution	Universiti Sains Malaysia
granting_department	Pusat Pengajian Sains Farmasi
publishDate	2014
url	http://eprints.usm.my/46371/1/Alireza%20Basiri24.pdf
_version_	1747821659037892608

Synthesis, Cholinesterase Inhibitory Activity And Molecular Docking Study Of Piperidone-Grafted Pyrimidine And Thiazolopyrimidine Derivatives

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