Yulya MARTYNENKO, Galına BEREST, Nına BUKHTIAYROVA, Igor BELENICHEV, Oleksıy VOSKOBOINIK, Sergıy KOVALENKO

2-[ 3-Aminoalkyl- alkaryl-,aryl- -1 H-1,2,4-triazol-5-yl]anilines: synthesis and anticonvulsant activity

The presented work is devoted to the development of synthesis methods for novel 2-[ 3-aminoalkyl- alkaryl-, aryl- -1$H$-1,2,4-triazolo]anilines. Abovementioned compounds were obtained via hydrazinolysis Ing-Manske procedure and acid hydrolysis of corresponding $N$-acylated { [1,2,4]triazolo[1,5-$c$]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-triazolo]anilines 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.

Keywords:

$N$-acylated{ [1, 2, 4]triazolo[1, 5-$c$]quinazolin-2-yl alkyl- alkaryl-, aryl- }amines, 2-[ 3-aminoalkyl- alkaryl- aryl- -1$H$-1, 2, 4-triazolo]anilines, hydrazinolysis, acidic hydrolysis, anticonvulsant activity,

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