The Chemotype of Chromanones as a Privileged Scaffold for Multineurotarget Anti-Alzheimer Agents
The Chemotype of Chromanones as a Privileged Scaffold for Multineurotarget Anti-Alzheimer Agents
Keuler, T.; Lemke, C.; Elsinghorst, P. W.; Iriepa, I.; Chioua, M.; Martínez-Grau, M. A.; Beadle, C. D.; Vetman, T.; López-Muñoz, F.; Wille, T.; Bartz, U.; Deuther-Conrad, W.; Marco-Contelles, J.; Gütschow, M.
Abstract
The multifactorial nature of Alzheimer’s disease necessitates the development of agents able to interfere with different relevant targets. A series of 22 tailored chromanones was conceptualized, synthesized and subjected to biological evaluation. We identified one representative bearing a linker-connected azepane moiety (compound 19) with balanced pharmacological properties. Compound 19 exhibited inhibitory activities against human acetyl-, butyrylcholinesterase and monoamine oxidase-B, as well as high affinity to both the 1 and 2 receptor. Our study provides a framework for the development of further chromanone-based multineurotarget agents.
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ACS Pharmacology & Translational Science 5(2022)11, 1097-1108
DOI: 10.1021/acsptsci.2c00097
Cited 2 times in Scopus
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Permalink: https://www.hzdr.de/publications/Publ-35194