Plys S. Synthesis, physical-chemical properties and pharmacological activity of the роtential neurotropic substanses - derivatives of the 1-R-5-аminо-1,2,3-triazol(1Н)-4-carboxylic acids та 1-R-1,2,3-triazol(1Н)-4,5-dicarboxylic acids

The target-directed synthesis of the potential anticonvulsants among the 1-R-5- amino-1,2,3-triazole(1H) derivatives was carried out. The preparative methods of synthesis of the new groups of biologically active compounds were designed: for anilides of the 1-R-5- amino-1,2,3-triazole(1H)-4-carboxylic acid - by interaction of the cуаnoacetic acid amides with the aryl azides under the homogenous basic catalysis conditions in the system methanol/sodium methylate; for derivatives of 1-R-1,2,3-triazol(1Н)-4,5-dicarboxylic acids - by the reaction of corresponding aryl azides with the acetylendicarboxylic acid or its methyl ester. The Dymrot's rearrangement (thermal isomerization) of 5-aminoderivatives into 5-arylamino derivatives was carried out. The structures of the synthesized compounds were confirmed by the elemental analysis, IR-, UV- and NMR-spectroscopy's data. The pharmacological screening showed the number of perspective anticonvulsants. For the most active one - dimethyl 1-phenyl-1,2,3-triazol(1Н)-4,5-dicarboxylate methods for quality control were developed in accordance with the modern requirements.