The Chemotype of Chromanones as a Privileged Scaffold for Multineurotarget Anti-Alzheimer Agents.
ACS Pharmacol Transl Sci
; 5(11): 1097-1108, 2022 Nov 11.
Article
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| MEDLINE
| ID: mdl-36407962
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 σ1 and σ2 receptors. Our study provides a framework for the development of further chromanone-based multineurotarget agents.
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MEDLINE
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En
Revista:
ACS Pharmacol Transl Sci
Año:
2022
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Article
País de afiliación:
Alemania