Publications Repository - Helmholtz-Zentrum Dresden-Rossendorf

1 Publication

Studies on the affinity of 6-[(: N -(cyclo)aminoalkyl)oxy]-4 H -chromen-4-ones for sigma 1/2 receptors

Deuther-Conrad, W.; Diez-Iriepa, D.; Iriepa, I.; López-Muñoz, F.; Martínez-Grau, A. M.; Gütschow, M.; Marco-Contelles, J.

Abstract

Sigma represent attractive targets for the development of potential agents for the treatment of neurodegenerative disorders. In search of multitarget small molecules (MSMs) against Morbus Alzheimer and related diseases, we have discovered that 6-(4-(piperidin-1-yl)butoxy)-4H-chromen-4-one (7), a previously identified MSM with potent dual-target activities against acetylcholinesterase and monoamine oxidase B, exhibited S1/S2 receptor modulatory activity. A further chromenone, 6-((5-morpholinopentyl)oxy)-4H-chromen-4-one (12), was identified to be almost equipotent to S1RA, an established 1 receptor antagonist.

Keywords: ADME; chromenones; docking; multitarget small molecules; radioligand assay; receptor binding; sigma 1/2 receptors

Permalink: https://www.hzdr.de/publications/Publ-31302


Years: 2023 2022 2021 2020 2019 2018 2017 2016 2015