Towards Alzheimer's disease-related targets: One-pot Cu(I)- mediated synthesis of new nitroindazolyltriazoles.
Cholinesterase inhibition
Click chemistry
CuAAC
In silico prediction
Nitroindazole
One-pot synthesis
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
01 2023
01 2023
Historique:
received:
18
08
2022
revised:
26
10
2022
accepted:
02
11
2022
pubmed:
19
11
2022
medline:
30
11
2022
entrez:
18
11
2022
Statut:
ppublish
Résumé
In this work, we have investigated the one pot strategy for the Cu(I)-mediated synthesis of new triazoles bearing nitroindazole moieties using different copper catalysts. The biological activity of newly synthesized nitroindazolyltriazoles towards Alzheimer's disease-related targets, namely cholinesterases, monoamine oxidases, and amyloid aggregation, were investigated. Predictions of target affinity, physicochemical parameters, gastrointestinal absorption and brain penetration were achieved by means of in silico tools.
Identifiants
pubmed: 36399866
pii: S0045-2068(22)00667-8
doi: 10.1016/j.bioorg.2022.106261
pii:
doi:
Substances chimiques
Amyloidogenic Proteins
0
Cholinesterases
EC 3.1.1.8
Monoamine Oxidase
EC 1.4.3.4
Indazoles
0
Triazoles
0
Copper
789U1901C5
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
106261Informations de copyright
Copyright © 2022 Elsevier Inc. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.