Record Details

Design, synthesis and evaluation of novel coumarin-oxa/thiadiazole hybrids as AChE inhibitors for the treatment of alzheimer's disease

NOPR - NISCAIR Online Periodicals Repository

View Archive Info
 
 
Field Value
 
Title Design, synthesis and evaluation of novel coumarin-oxa/thiadiazole hybrids as AChE inhibitors for the treatment of alzheimer's disease
 
Creator Jaber, Tasneem
More, Uttam A.
Sidat, Parin
Khan, Shabeena
Jain, Payal
N. Noolvi, Malleshappa
B. Palkar, Mahesh
 
Subject Coumarin derivatives
Molecular docking
Anti-Alzheimer Agents
 
Description 483-493
The most prevalent type of dementia is Alzheimer's disease. It is a central nervous system neurodegenerative disease
marked mostly by progressive cognitive dysfunction. One of the well-defined targets for Alzheimer's disease management is
the acetylcholinesterase enzyme. Coumarins are phytochemicals found naturally in many plant species that have a variety of
biological actions, including acetylcholinesterase inhibition. To accomplish this goal, several 7-hydroxy coumarin
derivatives as acetylcholinesterase (AChE) inhibitors have been synthesized using Pechmann condensation and conjugation
with various thiadiazole and oxadiazole. Spectral analysis has been used to characterize these molecules. An in silico
docking investigation against the AChE enzyme PDB 4EY7 demonstrates that the molecule interacts with the CAS and PAS
sites of the acetylcholinesterase enzyme. The coumarin moiety interacts with the PAS site, whereas the
thiadiazole/oxadiazole moiety interacts with the CAS site. Knowing the pharmacophoric requirements for inhibiting AChE,
compounds have been developed and evaluated for anti-Alzheimer efficacy in vitro utilizing the Ellman assay. With an IC50
of 0.75 μM, compound 9b have demonstrated great anti-Alzheimer efficacy. We conclude that the compounds described in
this paper can be used to develop novel anti-Alzheimer agents.
 
Date 2024-05-07T09:53:49Z
2024-05-07T09:53:49Z
2024-05
 
Type Article
 
Identifier 0975-0991 (Online); 0971-457X (Print)
http://nopr.niscpr.res.in/handle/123456789/63865
https://doi.org/10.56042/ijct.v31i3.3786
 
Language en
 
Publisher NIScPR-CSIR, India
 
Source IJCT Vol.31(3) [May 2024]