Details der Publikation - Synthesis, docking study, and biological evaluation of novel umbellipherone/hymecromone derivatives as acetylcholinesterase/butyrylcholinesterase inhibitors

Synthesis, docking study, and biological evaluation of novel umbellipherone/hymecromone derivatives as acetylcholinesterase/butyrylcholinesterase inhibitors

Abstract A novel hybrid series of umbellipherone and benzyl amine scaffolds, linked via triazole ring, was synthesized and evaluated as both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors. Most of the synthesized compounds showed moderate to high activities by using Ellman’s modified assay. Among the target compounds, 6e bearing 3-methoxy substituent on benzyl moiety was the most active one (AChE and BuChE $ IC_{50} $ = 3.4 and 1.1 μM, respectively). Finally, binding modes of the target compound was studied using molecular docking stimulations. The neuroprotectivity evaluation exhibited that this compound efficiently protected PC12 neurons against $ H_{2} $$ O_{2} $-induced cell death..

Medienart:	E-Artikel

Erscheinungsjahr:	2018
Erschienen:	2018

Enthalten in:	Zur Gesamtaufnahme - volume:27
Enthalten in:	Medicinal chemistry research - 27(2018), 7 vom: 30. Mai, Seite 1741-1747

Sprache:	Englisch

Beteiligte Personen:	Moradi, Alireza [VerfasserIn] Faraji, Laleh [VerfasserIn] Nadri, Hamid [VerfasserIn] Hasanpour, Zeinab [VerfasserIn] Moghadam, Farshad H [VerfasserIn] Pakseresht, Bahar [VerfasserIn] Golshani, Mostafa [VerfasserIn] Moghimi, Setareh [VerfasserIn] Ramazani, Ali [VerfasserIn] Firoozpour, Loghman [VerfasserIn] Khoobi, Mehdi [VerfasserIn] Foroumadi, Alireza [VerfasserIn]

Links:	Volltext [lizenzpflichtig]

Themen:	Alzheimer’s disease Cholinesterase inhibitor Docking Umbellipherone derivatives

Anmerkungen:	© Springer Science+Business Media, LLC, part of Springer Nature 2018

doi:	10.1007/s00044-018-2187-8

funding:
Förderinstitution / Projekttitel:

PPN (Katalog-ID):	OLC2096114721

Internformat


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Synthesis, docking study, and biological evaluation of novel umbellipherone/hymecromone derivatives as acetylcholinesterase/butyrylcholinesterase inhibitors

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