Title: A Boron-Chelating Piperazine-Tethered Schiff Base Can Modulate Excitability in Brain Slices in a Specific Frequency Range


BAŞOĞLU H., DEĞİRMENCİOĞLU İ., ÖZTÜRK H., Yorulmaz N., ABİDİN S., ABİDİN İ.

ChemistrySelect, vol.8, no.48, 2023 (SCI-Expanded) identifier

  • Publication Type: Article / Article
  • Volume: 8 Issue: 48
  • Publication Date: 2023
  • Doi Number: 10.1002/slct.202303410
  • Journal Name: ChemistrySelect
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier
  • Keywords: Boron, Brain slice, Epilepsy, Neurological agents, NMDA
  • Karadeniz Technical University Affiliated: Yes

Abstract

The ability of boron-containing compounds to make various bonds with biological targets draws attention in their use as new therapeutic agents. In this study, the effect of a newly synthesized molecule with the short name fmpemboron, “Difluoro [2-[([2-[4-(2,3,4-trimethoxybenzyl)piperazin-1-yl]ethyl] imino-κN)methyl]phenolato-κO]boron (5)”on the excitability of neurons in the brain was investigated for the first time. First of all, fmpemboron was synthesized and characterized. Secondly, virtual scanning of the molecule was performed using ADME and molecular docking methods. Then, epileptiform activities were induced in mouse brain slices using Mg-free or 4AP methods, and the effect of fmpemboron (5) at different concentrations was examined. The absorbance peak wavelength of fmpemboron (5) is between 330–340 nm and the fluorescence emission peak is 435 nm. According to ADME and molecular docking results, fmpemboron (5) can cross the blood-brain barrier (BBB) and has affinity for the NMDA receptor. It also significantly reduces the power of oscillations between 8–12 Hz and 13–29 Hz in epileptiform activities generated by the Mg-free method. Administration of 10 μM fmpemboron (5) had a modulatory effect on epileptiform activities, indicating that fmpemboron (5) can affect various neurological functions through NMDA channels. However, in-vivo dose-dependent studies are required to further investigate the effects of this novel molecule.