Triterpene-Based Carboxamides Act as Good Inhibitors of Butyrylcholinesterase.


Journal

Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009

Informations de publication

Date de publication:
07 Mar 2019
Historique:
received: 12 02 2019
revised: 25 02 2019
accepted: 02 03 2019
entrez: 15 3 2019
pubmed: 15 3 2019
medline: 27 6 2019
Statut: epublish

Résumé

A set of overall 40 carboxamides was prepared from five different natural occurring triterpenoids including oleanolic, ursolic, maslinic, betulinic, and platanic acid. All of which were derived from ethylene diamine holding an additional substituent connected to the ethylene diamine group. These derivatives were evaluated regarding their inhibitory activity of the enzymes acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) employing Ellman's assay. We further determined the type of inhibition and inhibition constants. Carboxamides derived from platanic acid have been shown to be potent and selective BChE inhibitors. Especially the mixed-type inhibitor (3β)-

Identifiants

pubmed: 30866589
pii: molecules24050948
doi: 10.3390/molecules24050948
pmc: PMC6429507
pii:
doi:

Substances chimiques

Cholinesterase Inhibitors 0
Triterpenes 0
platanic acid 6060-06-6
Acetylcholinesterase EC 3.1.1.7
Butyrylcholinesterase EC 3.1.1.8

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Références

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Auteurs

Anne Loesche (A)

Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany. anne.loesche@chemie.uni-halle.de.

Michael Kahnt (M)

Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany. michael.kahnt@chemie.uni-halle.de.

Immo Serbian (I)

Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany. immo.serbian@chemie.uni-halle.de.

Wolfgang Brandt (W)

Leibniz Institute of Plant Biochemistry, Bioorganic Chemistry, Weinberg 3, D-06120 Halle (Saale), Germany. wbrandt@ipb-halle.de.

René Csuk (R)

Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany. rene.csuk@chemie.uni-halle.de.

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Classifications MeSH