Journalartikel - Wissenschaftlicher Artikel | 2019 | Peer reviewed

Chromenones as Multineurotargeting Inhibitors of Human Enzymes

Autor*innen

Lemke, Carina ; Christmann, Joscha ; Yin, Jiafei ; Alonso, José M. ; Serrano, Estefanía ; Chioua, Mourad ; Ismaili, Lhassane ; Martínez-Grau, María Angeles ; Beadle, Christopher D. ; Vetman, Tatiana ; Dato, Florian M. ; Bartz, Ulrike ; Elsinghorst, Paul W. ; Pietsch, Markus ; Müller, Christa E. ; Iriepa, Isabel ; Wille, Timo ; Marco-Contelles, José ; Gütschow, Michael

Zeitschrift

ACS omega

DOI

10.1021/acsomega.9b03409

URL

http://pubs.acs.org/doi/pdf/10.1021/acsomega.9b03409

Weitere Details

Sprache

englisch

Darstellungsform

Text

Band

Ausgabe

Seitenbereich

22161 - 22168

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).

Zitierstile

Lemke, C., Christmann, J., Yin, J., Alonso, J. M., Serrano, E., Chioua, M., … Gütschow, M. (2019). Chromenones as Multineurotargeting Inhibitors of Human Enzymes. ACS Omega, 4(26), 22161–22168. doi:10.1021/acsomega.9b03409

In die Zwischenablage kopieren

Lemke, C., Christmann, J., Yin, J., Alonso, J.M., Serrano, E., Chioua, M., Ismaili, L., Martínez-Grau, M.A., Beadle, C.D., Vetman, T., Dato, F.M., Bartz, U., Elsinghorst, P.W., Pietsch, M., Müller, C.E., Iriepa, I., Wille, T., Marco-Contelles, J. and Gütschow, M., 2019. Chromenones as Multineurotargeting Inhibitors of Human Enzymes. ACS omega, [online] 4(26), pp.22161–22168. Available at: <http://pubs.acs.org/doi/pdf/10.1021/acsomega.9b03409>.

In die Zwischenablage kopieren

Lemke, Carina u. a. 2019. Chromenones as Multineurotargeting Inhibitors of Human Enzymes. ACS omega 4, 26, 22161–22168. http://pubs.acs.org/doi/pdf/10.1021/acsomega.9b03409.

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Zitierstile

In die Zwischenablage kopieren

Lemke, Carina u. a. 2019. Chromenones as Multineurotargeting Inhibitors of Human Enzymes. ACS omega 4, 26, 22161–22168. http://pubs.acs.org/doi/pdf/10.1021/acsomega.9b03409.

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American Psychological Association 6th edition (DOI)

Anglia Ruskin University - Harvard

Gesellschaft für Bildung und Forschung in Europa - Harvard