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New Hybrid Structures Based on Memanthine and Edaravone Molecules.

V V Grigoriev1, E F Shevtsova2, A Yu Aksinenko2

  • 1Institute of Physiologically Active Substances, Federal Research Center for Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, Chernogolovka, Moscow oblast, Russia. grigor@ipac.ac.ru.

Doklady. Biochemistry and Biophysics
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PubMed
Summary

New hybrid molecules combining memantine and edaravone were synthesized. These compounds act as dual N-methyl-D-aspartate (NMDA) receptor blockers and inhibit lipid peroxidation, offering potential therapeutic advantages.

Keywords:
1-aminoadamantanesAlzheimer’s diseaseNMDA receptorsamyotrophic lateral sclerosisedaravonelipid peroxidationmemantineoxidative stress

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Area of Science:

  • Medicinal Chemistry
  • Neuroscience
  • Pharmacology

Background:

  • Memantine is an N-methyl-D-aspartate (NMDA) receptor antagonist used for Alzheimer's disease.
  • Edaravone is a neuroprotective agent that inhibits lipid peroxidation.
  • NMDA receptors play a crucial role in excitotoxicity and neurodegenerative diseases.

Purpose of the Study:

  • To synthesize novel hybrid molecules integrating memantine and edaravone functionalities.
  • To investigate the NMDA receptor blocking properties of these hybrids at both intrachannel and allosteric sites.
  • To evaluate the lipid peroxidation inhibitory activity of the synthesized compounds.

Main Methods:

  • Chemical synthesis of hybrid molecules linking pyrazolone and adamantane fragments via an alkyl linker.
  • Pharmacological evaluation of NMDA receptor antagonism, including intrachannel and allosteric site blockade.
  • In vitro assessment of lipid peroxidation inhibition.

Main Results:

  • Successful synthesis of novel hybrid structures based on memantine and edaravone.
  • The hybrid compounds demonstrated dual-site NMDA receptor blockade (intrachannel and allosteric), a property absent in parent drugs.
  • One hybrid compound exhibited significant lipid peroxidation inhibitory activity, comparable to edaravone.

Conclusions:

  • The novel hybrid molecules possess dual-site NMDA receptor antagonist properties.
  • These hybrids combine the neuroprotective effects of edaravone with enhanced NMDA receptor modulation.
  • The most active compound shows promise as a multi-target therapeutic agent for neurodegenerative conditions.