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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 IC(50) value of 1.57 µM against ac...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2015
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272427/ https://www.ncbi.nlm.nih.gov/pubmed/25642838 http://dx.doi.org/10.3390/molecules20022296 |
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author | Almansour, Abdulrahman I. Suresh Kumar, Raju Arumugam, Natarajan Basiri, Alireza Kia, Yalda Ali, Mohamed Ashraf Farooq, Mehvish Murugaiyah, Vikneswaran |
author_facet | Almansour, Abdulrahman I. Suresh Kumar, Raju Arumugam, Natarajan Basiri, Alireza Kia, Yalda Ali, Mohamed Ashraf Farooq, Mehvish Murugaiyah, Vikneswaran |
author_sort | Almansour, Abdulrahman I. |
collection | PubMed |
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 IC(50) 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. |
format | Online Article Text |
id | pubmed-6272427 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2015 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62724272018-12-13 A Facile Ionic Liquid Promoted Synthesis, Cholinesterase Inhibitory Activity and Molecular Modeling Study of Novel Highly Functionalized Spiropyrrolidines Almansour, Abdulrahman I. Suresh Kumar, Raju Arumugam, Natarajan Basiri, Alireza Kia, Yalda Ali, Mohamed Ashraf Farooq, Mehvish Murugaiyah, Vikneswaran Molecules Article 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 IC(50) 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. MDPI 2015-01-29 /pmc/articles/PMC6272427/ /pubmed/25642838 http://dx.doi.org/10.3390/molecules20022296 Text en © 2015 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Almansour, Abdulrahman I. Suresh Kumar, Raju Arumugam, Natarajan Basiri, Alireza Kia, Yalda Ali, Mohamed Ashraf Farooq, Mehvish Murugaiyah, Vikneswaran A Facile Ionic Liquid Promoted Synthesis, Cholinesterase Inhibitory Activity and Molecular Modeling Study of Novel Highly Functionalized Spiropyrrolidines |
title | 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_short | 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 |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272427/ https://www.ncbi.nlm.nih.gov/pubmed/25642838 http://dx.doi.org/10.3390/molecules20022296 |
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