Novel 12-hydroxydehydroabietylamine derivatives act as potent and selective butyrylcholinesterase inhibitors.
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
09 2019
09 2019
Historique:
received:
06
01
2019
revised:
23
06
2019
accepted:
26
06
2019
pubmed:
8
7
2019
medline:
21
10
2020
entrez:
8
7
2019
Statut:
ppublish
Résumé
The skeleton of the diterpene dehydroabietylamine was modified, and a set of 12-hydroxy-dehydroabietylamine derivatives was obtained. The compounds were screened in colorimetric Ellman's assays to determine their ability to act as inhibitors for the enzymes acetylcholinesterase (AChE, from electric eel) and butyrylcholinesterase (BChE, from equine serum). Additional investigations concerning the enzyme kinetics were performed and showed 12-hydroxy-N-(4-nitro-benzoyl)dehydroabietylamine (13) and 12-hydroxy-N-(isonicotinoyl)dehydroabietylamine (17) as selective BChE inhibitors holding good inhibition constants K
Identifiants
pubmed: 31280014
pii: S0045-2068(19)30021-5
doi: 10.1016/j.bioorg.2019.103092
pii:
doi:
Substances chimiques
12-Hydroxy-N-(isonicotinoyl)dehydroabietylamine
0
Cholinesterase Inhibitors
0
Diterpenes
0
Ethylamines
0
Acetylcholinesterase
EC 3.1.1.7
Butyrylcholinesterase
EC 3.1.1.8
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
103092Informations de copyright
Copyright © 2019 Elsevier Inc. All rights reserved.