A PHP Error was encountered

Severity: Warning

Message: file_get_contents(https://...@pubfacts.com&api_key=b8daa3ad693db53b1410957c26c9a51b4908&a=1): Failed to open stream: HTTP request failed! HTTP/1.1 429 Too Many Requests

Filename: helpers/my_audit_helper.php

Line Number: 176

Backtrace:

File: /var/www/html/application/helpers/my_audit_helper.php
Line: 176
Function: file_get_contents

File: /var/www/html/application/helpers/my_audit_helper.php
Line: 250
Function: simplexml_load_file_from_url

File: /var/www/html/application/helpers/my_audit_helper.php
Line: 1034
Function: getPubMedXML

File: /var/www/html/application/helpers/my_audit_helper.php
Line: 3152
Function: GetPubMedArticleOutput_2016

File: /var/www/html/application/controllers/Detail.php
Line: 575
Function: pubMedSearch_Global

File: /var/www/html/application/controllers/Detail.php
Line: 489
Function: pubMedGetRelatedKeyword

File: /var/www/html/index.php
Line: 316
Function: require_once

Aryldiazoquinoline based multifunctional small molecules for modulating Aβ aggregation and cholinesterase activity related to Alzheimer's disease. | LitMetric

Research continues to find a breakthrough for the treatment of Alzheimer's Disease (AD) due to its complicated pathology. Presented herein is a novel series of arydiazoquinoline molecules investigated for their multifunctional properties against the factors contributing to Alzheimer's disease (AD). The inhibitory properties of fourteen closely related aryldiazoquinoline derivatives have been evaluated for their inhibitory effect on Aβ peptide aggregation. Most of these molecules inhibited Aβ fibrillation by 50-80%. Selected molecules were also investigated for their binding behaviour to preformed Aβ aggregates indicating a nanomolar affinity. In addition, these compounds were further investigated as cholinesterase inhibitors. Interestingly, some of the compounds turned out to be moderate inhibitors for AChE activity with IC values in low micro molar range. The highest anti-AChE activity was shown by compound labelled as 2a with an IC value of 6.2 μM followed by 2b with IC value of 7.0 μM. In order to understand the inhibitory effect, binding of selected molecules to AChE enzyme was studied using molecular docking. In addition, cell toxicity studies using Neuro2a cells were performed to assess their effect on neuronal cell viability which suggests that these molecules possess a non-toxic molecular framework. Overall, the study identifies a family of molecules that show good anti-Aβ-aggregation properties and moderately inhibit cholinesterase activity.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9055851PMC
http://dx.doi.org/10.1039/d0ra05172aDOI Listing

Publication Analysis

Top Keywords

alzheimer's disease
12
cholinesterase activity
8
molecules investigated
8
selected molecules
8
molecules
7
aryldiazoquinoline based
4
based multifunctional
4
multifunctional small
4
small molecules
4
molecules modulating
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!