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Chromenones as Multineurotargeting Inhibitors of Human Enzymes

  • The complex nature of multifactorial diseases, such as Morbus Alzheimer, has produced a strong need to design multitarget-directed ligands to address the involved complementary pathways. We performed a purposive structural modification of a tetratarget small-molecule, that is contilisant, and generated a combinatorial library of 28 substituted chromen-4-ones. The compounds comprise a basic moiety which is linker-connected to the 6-position of the heterocyclic chromenone core. The syntheses were accomplished by Mitsunobu- or Williamson-type ether formations. The resulting library members were evaluated at a panel of seven human enzymes, all of which being involved in the pathophysiology of neurodegeneration. A concomitant inhibition of human acetylcholinesterase and human monoamine oxidase B, with IC50 values of 5.58 and 7.20 μM, respectively, was achieved with the dual-target 6-(4-(piperidin-1-yl)butoxy)-4H-chromen-4-one (7).

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Document Type:Article
Author:Carina Lemke, Joscha Christmann, Jiafei Yin, José M. Alonso, Estefanía Serrano, Mourad Chioua, Lhassane Ismaili, María Angeles Martínez-Grau, Christopher D. Beadle, Tatiana Vetman, Florian M. Dato, Ulrike Bartz, Paul W. Elsinghorst, Markus Pietsch, Christa E. Müller, Isabel Iriepa, Timo Wille, José Marco-Contelles, Michael Gütschow
Parent Title (English):ACS Omega
First Page:21636
Last Page:22260
Pubmed Id:
Publisher:American Chemical Society (ACS)
Publishing Institution:Hochschule Bonn-Rhein-Sieg
Date of first publication:2019/12/11
© 2019 American Chemical Society. This is an open access article published under an ACS AuthorChoice License, which permits copying and redistribution of the article or any adaptations for non-commercial purposes.
Departments, institutes and facilities:Fachbereich Angewandte Naturwissenschaften
Dewey Decimal Classification (DDC):5 Naturwissenschaften und Mathematik / 57 Biowissenschaften; Biologie / 570 Biowissenschaften; Biologie
Entry in this database:2019/12/14
Licence (English):License LogoACS AuthorChoice/Editors’ Choice License