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Chemical Papers

, Volume 73, Issue 2, pp 509–515 | Cite as

Effect on AMPA receptors and lipophilicity of substituted pyridoindoles as potential neuroprotectors

  • Svetlana Blokhina
  • Marina Ol’khovich
  • Angelica SharapovaEmail author
Original Paper
  • 14 Downloads

Abstract

The effect of the chemical nature of substituents (–H, –CH3–, –OCH3, –F and –Cl) introduced into the tricyclic fragment of hydrogenated pyrido[4,3-b]indoles on the compounds ability to positively modulate the activity of ionotropic glutamate AMPA receptors have been studied. The unsubstituted derivative, compounds with a methyl group and a fluorine atom were found to have the highest bioactivity in this test. The partition coefficients of the synthesized derivatives in the system 1-octanol/buffer pH 7.4 in the temperature range of 293.15–313.15 K have been measured. It has been found that as the lipophilicity of the compounds studied increases, the maximum biological activity is achieved at a higher concentration of the administered substance. The thermodynamic transfer functions of the studied substances from aqueous medium to organic phase have been calculated.

Keywords

Derivatives of Dimebon Bioactivity 1-Octanol/buffer pH 7.4 system Partition coefficient Transfer thermodynamics 

Notes

Acknowledgements

This work was supported by the grant of RFBR no. 18-43-370016.

Compliance with ethical standards

Conflict of interest

The authors report that there are no conflicts of interest in this article.

Supplementary material

11696_2018_595_MOESM1_ESM.xls (48 kb)
Supplementary material 1 (XLS 48 kb)

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Copyright information

© Institute of Chemistry, Slovak Academy of Sciences 2018

Authors and Affiliations

  • Svetlana Blokhina
    • 1
  • Marina Ol’khovich
    • 1
  • Angelica Sharapova
    • 1
    Email author
  1. 1.Institute of Solution ChemistryRussian Academy of SciencesIvanovoRussia

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