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

Svetlana Blokhina, Marina Ol’khovich, and Angelica Sharapova

Russian Academy of Sciences, Ivanovo, Russia

 

E-mail: avs@isc-ras.ru

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 

Full paper is available at www.springerlink.com.

DOI: 10.1007/s11696-018-0595-3

 

Chemical Papers 73 (2) 509–515 (2019)

Tuesday, June 18, 2024

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