New Hybrid Structures Based on Memanthine and Edaravone Molecules

V. V. Grigoriev, E. F. Shevtsova,A. Yu. Aksinenko, I. M. Veselov, T. V. Goreva, A. V. Gabrelyan, S. O. Bachurin

DOKLADY BIOCHEMISTRY AND BIOPHYSICS(2023)

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摘要
New hybrid structures based on memantine and edaravone molecules, in which the pyrazolone ring and adamantane fragments are linked by an alkyl linker, were synthesized. It was found that, in addition to the ability to block the intrachannel site of NMDA receptors, the new hybrid compounds exhibit the property of blockers of the allosteric site of NMDA receptors, which is not inherent in memantine and edaravone preparations. The most active hit compound was determined, which, along with the properties of a two-site blocker of the NMDA receptor, exhibits a pronounced activity as an inhibitor of lipid peroxidation, similarly to the drug edaravone.
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关键词
amyotrophic lateral sclerosis,Alzheimer's disease,memantine,edaravone,1-aminoadamantanes,NMDA receptors,oxidative stress,lipid peroxidation
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