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A facile ionic liquid promoted synthesis, cholinesterase inhibitory activity and molecular modeling study of novel highly functionalized spiropyrrolidines

Almansour AI 1 , Kumar RS 2 , Arumugam N 3 , Basiri A 4 , Kia Y 5 , Ali MA 6 Show all authors , Farooq M 7 , Murugaiyah V 8

Affiliations 

  • 1 Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia. almansor@ksu.edu.sa
  • 2 Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia. sraju@ksu.edu.sa
  • 3 Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia. aruorgchem@gmail.com
  • 4 School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden 11800, Malaysia. diba115920@gmail.com
  • 5 School of Chemical Sciences, Universiti Sains Malaysia, Minden 11800, Malaysia. kia.yalda@yahoo.com
  • 6 Pharmacogenetic and Novel Therapeutic Institute for Research in Molecular Medicine, Universiti Sains Malaysia, Minden 11800, Malaysia. asraf80med@yahoo.com
  • 7 Institute of Pharmaceutical Science, King's College London, London SE1 9NH, UK. Mehvish.farooq@kcl.ac.uk
  • 8 School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden 11800, Malaysia. vicky@usm.my
Molecules, 2015 Jan 29;20(2):2296-309.
PMID: 25642838 DOI: 10.3390/molecules20022296

Abstract

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.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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