Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking

Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of ChEs is considered to be involved in increasing acetylcholine level in the brain and thus has been implicated in the treatment of Alzheimer’s disease. We have designed and synthesized a series o...

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Main Authors:	Yar, Muhammad, Bajda, Marek, Mehmood, Rana Atif, Sidra, Lala Rukh, Ullah, Nisar, Shahzadi, Lubna, Ashraf, Muhammad, Ismail, Tayaba, Shahzad, Sohail Anjum, Khan, Zulfiqar Ali, Naqvi, Syed Ali Raza, Mahmood, Nasir
Format:	Online
Language:	English
Published:	Bentham Science Publishers Ltd 2014
Online Access:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3977535/

id	pubmed-3977535
recordtype	oai_dc
spelling	pubmed-39775352014-04-07 Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking Yar, Muhammad Bajda, Marek Mehmood, Rana Atif Sidra, Lala Rukh Ullah, Nisar Shahzadi, Lubna Ashraf, Muhammad Ismail, Tayaba Shahzad, Sohail Anjum Khan, Zulfiqar Ali Naqvi, Syed Ali Raza Mahmood, Nasir Article Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of ChEs is considered to be involved in increasing acetylcholine level in the brain and thus has been implicated in the treatment of Alzheimer’s disease. We have designed and synthesized a series of novel indole derivatives and screened them for inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Most of the tested compounds exhibited inhibitory activity against AChE and BChE. Among them 4f and 6e showed the highest AChE inhibitory activity with IC50 91.21±0.06 and 68.52±0.04 μM, respectively. However compound 5a exhibited the highest inhibitory activity against BChE (IC50 55.21±0.12 μM). Bentham Science Publishers Ltd 2014-03 2014-03 /pmc/articles/PMC3977535/ /pubmed/24719609 http://dx.doi.org/10.2174/15701808113106660078 Text en © 2014 Bentham Science Publishers Ltd. http://creativecommons.org/licenses/by/2.5/ This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.5/), which permits unrestrictive use, distribution, and reproduction in any medium, provided the original work is properly cited.
repository_type	Open Access Journal
institution_category	Foreign Institution
institution	US National Center for Biotechnology Information
building	NCBI PubMed
collection	Online Access
language	English
format	Online
author	Yar, Muhammad Bajda, Marek Mehmood, Rana Atif Sidra, Lala Rukh Ullah, Nisar Shahzadi, Lubna Ashraf, Muhammad Ismail, Tayaba Shahzad, Sohail Anjum Khan, Zulfiqar Ali Naqvi, Syed Ali Raza Mahmood, Nasir
spellingShingle	Yar, Muhammad Bajda, Marek Mehmood, Rana Atif Sidra, Lala Rukh Ullah, Nisar Shahzadi, Lubna Ashraf, Muhammad Ismail, Tayaba Shahzad, Sohail Anjum Khan, Zulfiqar Ali Naqvi, Syed Ali Raza Mahmood, Nasir Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking
author_facet	Yar, Muhammad Bajda, Marek Mehmood, Rana Atif Sidra, Lala Rukh Ullah, Nisar Shahzadi, Lubna Ashraf, Muhammad Ismail, Tayaba Shahzad, Sohail Anjum Khan, Zulfiqar Ali Naqvi, Syed Ali Raza Mahmood, Nasir
author_sort	Yar, Muhammad
title	Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking
title_short	Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking
title_full	Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking
title_fullStr	Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking
title_full_unstemmed	Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking
title_sort	design and synthesis of new dual binding site cholinesterase inhibitors: in vitro inhibition studies with in silico docking
description	Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of ChEs is considered to be involved in increasing acetylcholine level in the brain and thus has been implicated in the treatment of Alzheimer’s disease. We have designed and synthesized a series of novel indole derivatives and screened them for inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Most of the tested compounds exhibited inhibitory activity against AChE and BChE. Among them 4f and 6e showed the highest AChE inhibitory activity with IC50 91.21±0.06 and 68.52±0.04 μM, respectively. However compound 5a exhibited the highest inhibitory activity against BChE (IC50 55.21±0.12 μM).
publisher	Bentham Science Publishers Ltd
publishDate	2014
url	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3977535/
_version_	1612074820938235904

Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking

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