A Facile Ionic Liquid Promoted Synthesis, Cholinesterase Inhibitory Activity and Molecular Modeling Study of Novel Highly Functionalized Spiropyrrolidines

A Facile Ionic Liquid Promoted Synthesis, Cholinesterase Inhibitory Activity and Molecular Modeling Study of Novel Highly Functionalized Spiropyrrolidines

A series of novel dimethoxyindanone embedded spiropyrrolidines were synthesized in ionic liquid, [bmim]Br and were evaluated for their inhibitory activities towards cholinesterases. Among the spiropyrrolidines, compound 4f exhibited the most potent activity with an IC50 value of 1.57 µM against acet...

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Main Authors: Abdulrahman I. Almansour, Raju Suresh Kumar, Natarajan Arumugam, Alireza Basiri, Yalda Kia, Mohamed Ashraf Ali, Mehvish Farooq, Vikneswaran Murugaiyah
Format: Article
Language:English
Published: MDPI AG 2015-01-01
Series:Molecules
Subjects:
acetylcholinesterase (AChE), butyrylcholinesterase (BChE), Alzheimer’s disease (AD), spiropyrrolidines, ionic liquid and molecular docking study
Online Access:http://www.mdpi.com/1420-3049/20/2/2296
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spelling doaj-3dc95383393142f58e8968d06589e1552020-11-24T23:09:04ZengMDPI AGMolecules1420-30492015-01-012022296230910.3390/molecules20022296molecules20022296A Facile Ionic Liquid Promoted Synthesis, Cholinesterase Inhibitory Activity and Molecular Modeling Study of Novel Highly Functionalized SpiropyrrolidinesAbdulrahman I. Almansour0Raju Suresh Kumar1Natarajan Arumugam2Alireza Basiri3Yalda Kia4Mohamed Ashraf Ali5Mehvish Farooq6Vikneswaran Murugaiyah7Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi ArabiaDepartment of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi ArabiaDepartment of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi ArabiaSchool of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden 11800, MalaysiaSchool of Chemical Sciences, Universiti Sains Malaysia, Minden 11800, MalaysiaPharmacogenetic and Novel Therapeutic Institute for Research in Molecular Medicine, Universiti Sains Malaysia, Minden 11800, MalaysiaInstitute of Pharmaceutical Science, King's College London, London SE1 9NH, UKSchool of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden 11800, MalaysiaA series of novel dimethoxyindanone embedded spiropyrrolidines were synthesized in ionic liquid, [bmim]Br and were evaluated for their inhibitory activities towards cholinesterases. Among the spiropyrrolidines, compound 4f exhibited the most potent activity with an IC50 value of 1.57 µM against acethylcholinesterase (AChE). Molecular docking simulation for the most active compound was employed with the aim of disclosing its binding mechanism to the active site of AChE receptor.http://www.mdpi.com/1420-3049/20/2/2296acetylcholinesterase (AChE), butyrylcholinesterase (BChE), Alzheimer’s disease (AD), spiropyrrolidines, ionic liquid and molecular docking study
collection DOAJ
language English
format Article
sources DOAJ
author Abdulrahman I. Almansour
Raju Suresh Kumar
Natarajan Arumugam
Alireza Basiri
Yalda Kia
Mohamed Ashraf Ali
Mehvish Farooq
Vikneswaran Murugaiyah
spellingShingle Abdulrahman I. Almansour
Raju Suresh Kumar
Natarajan Arumugam
Alireza Basiri
Yalda Kia
Mohamed Ashraf Ali
Mehvish Farooq
Vikneswaran Murugaiyah
A Facile Ionic Liquid Promoted Synthesis, Cholinesterase Inhibitory Activity and Molecular Modeling Study of Novel Highly Functionalized Spiropyrrolidines
Molecules
acetylcholinesterase (AChE), butyrylcholinesterase (BChE), Alzheimer’s disease (AD), spiropyrrolidines, ionic liquid and molecular docking study
author_facet Abdulrahman I. Almansour
Raju Suresh Kumar
Natarajan Arumugam
Alireza Basiri
Yalda Kia
Mohamed Ashraf Ali
Mehvish Farooq
Vikneswaran Murugaiyah
author_sort Abdulrahman I. Almansour
title A Facile Ionic Liquid Promoted Synthesis, Cholinesterase Inhibitory Activity and Molecular Modeling Study of Novel Highly Functionalized Spiropyrrolidines
title_short A Facile Ionic Liquid Promoted Synthesis, Cholinesterase Inhibitory Activity and Molecular Modeling Study of Novel Highly Functionalized Spiropyrrolidines
title_full A Facile Ionic Liquid Promoted Synthesis, Cholinesterase Inhibitory Activity and Molecular Modeling Study of Novel Highly Functionalized Spiropyrrolidines
title_fullStr A Facile Ionic Liquid Promoted Synthesis, Cholinesterase Inhibitory Activity and Molecular Modeling Study of Novel Highly Functionalized Spiropyrrolidines
title_full_unstemmed A Facile Ionic Liquid Promoted Synthesis, Cholinesterase Inhibitory Activity and Molecular Modeling Study of Novel Highly Functionalized Spiropyrrolidines
title_sort facile ionic liquid promoted synthesis, cholinesterase inhibitory activity and molecular modeling study of novel highly functionalized spiropyrrolidines
publisher MDPI AG
series Molecules
issn 1420-3049
publishDate 2015-01-01
description A series of novel dimethoxyindanone embedded spiropyrrolidines were synthesized in ionic liquid, [bmim]Br and were evaluated for their inhibitory activities towards cholinesterases. Among the spiropyrrolidines, compound 4f exhibited the most potent activity with an IC50 value of 1.57 µM against acethylcholinesterase (AChE). Molecular docking simulation for the most active compound was employed with the aim of disclosing its binding mechanism to the active site of AChE receptor.
topic acetylcholinesterase (AChE), butyrylcholinesterase (BChE), Alzheimer’s disease (AD), spiropyrrolidines, ionic liquid and molecular docking study
url http://www.mdpi.com/1420-3049/20/2/2296
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