2-(3-Aminoalkyl-(alkaryl-,aryl-))-1 H -1,2,4-triazol-5-ylanilines: synthesis and anticonvulsant activity

摘要

The presented work is devoted to the development of synthesis methods for novel 2-(3-aminoalkyl-(alkaryl-, aryl-))-1$H$-1,2,4-triazoloanilines. Abovementioned compounds were obtained via hydrazinolysis (Ing-Manske procedure) and acid hydrolysis of corresponding $N$-acylated {(1,2,4triazolo1,5-$c$quinazolin-2-yl)alkyl-(alkaryl-, aryl-)} amines. The regioselectivity of hydrazinolysis and hydrolysis were established. The features of spectral characteristics were studied and discussed. Characteristic patterns of protons signals splitting in $^{1}$H NMR of the synthesized compounds were established. The effect of the synthesized compounds on the pentylenetetrazol seizures was studied. It was found that according to some indicators, anticonvulsant activity of 2-(3-aminoalkyl-(alkaryl-, aryl-))-1$H$-1,2,4-triazoloanilines superior or comparable with effect of the reference drug "Lamotrigine". It is a valid argument for their further structural modification, in-depth study of activity mechanisms and further study of anticonvulsant activity on other experimental seizures models.