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

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

Pages : 746-755

View : 17 | Download : 3

Publication Date : 0000-00-00

Article Type : Research Paper

Abstract :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