Format

Send to

Choose Destination
Chem Biol Drug Des. 2017 May;89(5):783-789. doi: 10.1111/cbdd.12902. Epub 2016 Dec 11.

Synthesis and anticholinesterase activity of new substituted benzo[d]oxazole-based derivatives.

Author information

1
Department of Chemistry, Faculty of Science, Shahid Bahonar University of Kerman, Kerman, Iran.
2
Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran.
3
Department of Medicinal Chemistry, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran.
4
Department of Medicinal Chemistry, Faculty of Pharmacy and Neuroscience Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran.
5
Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran.

Abstract

A series of novel benzo[d]oxazole derivatives (6a-n) have been synthesized and biologically evaluated as potential inhibitors of acetylcholinesterases (AChE) and butyrylcholinesterase (BChE). The chemical structures of all final compounds were confirmed by spectroscopic methods. In vitro studies showed that most of the synthesized compounds are potent acetylcholinesterase and butyrylcholinesterase inhibitors. Among them, compounds 6a and 6j strongly inhibited AChE and BChE activities with IC50 values of 1.03-1.35 and 6.6-8.1 μm, respectively. Docking studies also provided the binding modes of action and identified hydrophobic pi forces as the main interaction.

KEYWORDS:

Alzheimer's disease; acetylcholinesterase; benzo[d]oxazol; docking study

PMID:
27863021
DOI:
10.1111/cbdd.12902
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Wiley
Loading ...
Support Center