Severina G. Synthesis, physical-chemical properties and anticonvulsant activity of the 3-amino- and 4-amino-3-mercapto-1,2,4-triazole derivatives and products of their chemicals transformations.

The target-directed synthesis of the potential anticonvulsants among the 3-amino- and 4-amino-3-mercapto-1,2,4-triazole has been carried out. The preparative methods of the synthesis of the new groups of biologically active compounds were developed: derivatives of [1,2,4]triazolo[1,5-а]pyrimidine, [1,2,4]triazolo[4,3-b]pyridazin-3-ylthio-acetic acid and its amides, N-aryl-2-[4-(1Н-1-pyrrolyl)-4Н-1,2,4-triazol-3- ylthio]acetamides, 7Н-1,2,4-triazolo[3,4-b][1,3,4]thiadiazine.The structure of the compounds synthesized have been confirmed by the data of the elemental analysis, NMR spectroscopy, chromatographic mass spectrometry, and in some cases by the X-ray diffraction analysis and counter synthesis. Pharmacological activity of the substances synthesized has been prognosed with the PASS-program. The pharmacological screening showed the number of perspective anticonvulsants. For the most active one - 3-chloro-4-methoxy anilide of the 1-(2'-fluorophenyl)-5-methyl-1,2,3-triazole(1H)-4-carboxylic acid has been recommended for preclinical biological researches as potential preparation with anticonvulsive action.