Journal
ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE
Volume 5, Issue 11, Pages 1097-1108Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsptsci.2c000971097
Keywords
chromanones; Alzheimer?s disease; multineurotarget agents; ? 1 and ?2 receptors; monoamine oxidases; human cholinesterases
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Funding
- Jurgen Manchot Foundation, Dusseldorf, Germany
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The multifactorial nature of Alzheimer's disease requires the development of drugs that can target different relevant pathways. In this study, we synthesized a series of tailored chromanones and identified compound 19 as a representative compound with balanced pharmacological properties. Compound 19 showed inhibitory activities against human acetyl- and butyrylcholinesterase, monoamine oxidase-B, and high affinity to sigma 1 and sigma 2 receptors.
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 sigma 1 and sigma 2 receptors. Our study provides a framework for the development of further chromanone-based
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