Tacrine-xanomeline and tacrine-iperoxo hybrid ligands: Synthesis and biological evaluation at acetylcholinesterase and M
Acetylcholinesterase
/ metabolism
Allosteric Regulation
/ drug effects
Animals
CHO Cells
Cholinesterase Inhibitors
/ chemistry
Cricetulus
Electrophorus
Humans
Isoxazoles
/ chemical synthesis
Ligands
Molecular Docking Simulation
Pyridines
/ chemical synthesis
Quaternary Ammonium Compounds
/ chemical synthesis
Receptor, Muscarinic M1
/ agonists
Tacrine
/ analogs & derivatives
Thiadiazoles
/ chemical synthesis
Allosteric modulation
Bitopic ligands
Ellman’s assay
Inositol monophosphate
Iperoxo
M(1) muscarinic acetylcholine receptor
Multitarget compounds
Phospholipase C
Tacrine
Xanomeline
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
03 2020
03 2020
Historique:
received:
19
09
2019
revised:
20
12
2019
accepted:
28
01
2020
pubmed:
8
2
2020
medline:
25
2
2021
entrez:
8
2
2020
Statut:
ppublish
Résumé
We synthesized a set of new hybrid derivatives (7-C8, 7-C10, 7-C12 and 8-C8, 8-C10, 8-C12), in which a polymethylene spacer chain of variable length connected the pharmacophoric moiety of xanomeline, an M
Identifiants
pubmed: 32032848
pii: S0045-2068(19)31569-X
doi: 10.1016/j.bioorg.2020.103633
pii:
doi:
Substances chimiques
Cholinesterase Inhibitors
0
Isoxazoles
0
Ligands
0
Pyridines
0
Quaternary Ammonium Compounds
0
Receptor, Muscarinic M1
0
Thiadiazoles
0
iperoxo
0
Tacrine
4VX7YNB537
xanomeline
9ORI6L73CJ
Acetylcholinesterase
EC 3.1.1.7
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
103633Informations de copyright
Copyright © 2020 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.