SYNTHESIS, STRUCTURE AND PHARMACOLOGICAL EVALUATION OF 1-(1H-PYRROL-1-YLMETHYL)-4-AZATRICYCLO[5.2.1.0(2,6)] DEC-8-ENE-3,5-DIONE.

A set of arylpiperazine derivatives with imide fragments, 1-(1H-pyrrol-1-ylmethyl)-10-oxa-4-azatricyclo[5.2.1.

Biological activity of novel N-substituted amides of endo-3-(3-methylthio-1,2,4-triazol-5-yl)bicyclo[2.2.1]hept-5-ene-2-carboxylic acid and N-substituted amides of 1-(5-methylthio-1,2,4-triazol-3-yl)cyclohexane-2-carboxylic acids.

N-Substituted amides of endo-3-(3-methylthio-1,2,4-triazol-5-yl)bicyclo[2.2.1]hept-5-ene-2-carboxylic acid and 1-(5-methylthio-1,2,4-triazol-3-yl)cyclohexane-2-carboxylic acid were prepared by the condensation reaction of endo-S-methyl-N1-(bicyclo[2.

Pharmacological study on some new 3-[(1-methylpyrrol-2-yl)-methyl]-4-substituted 4,5-dihydro-1H-1,2,4-triazol-5-ones.

3-[(1-Methylpyrrol-2-yl)methyl]-4-substituted 4,5-dihydro-1H-1,2,4-triazol-5-ones were obtained by the cyclization reaction of 1-[(1-methylpyrrol-2-yl)acetyl]-4-substituted semicarbazides in alkaline medium. The effects of the synthesized compounds of the central nervous system of mice were studied.

Synthesis of amides of 2,4-dioxothiazolidin-5-yl acetic acid with 1,2,4-triazole substituents.

In the reaction of (2,4-dioxothiazolidin-5-yl)acetyl chloride with 1,2,4-triazole, 4-phenyl-1,2,4-triazolin-5-one and 4-phenyl-1,2,4-triazolin-5-thione, the new corresponding amides (2-4) were obtained. For compounds 2 and 4 effects on central nervous system (CNS) of mice were studied.

Synthesis and biological activity of new derivatives of 3-phenoxymethyl-4-R-D2-1,2,4-triazoline-5-thione.

New derivatives of 1,2,4-triazoline-5-thione system were obtained. The effects of both these compounds AP-I (3-phenoxymethyl-4-phenyl-D2-1,2,4-triazoline-5-thione) and AP-II (3-phenoxymethyl-4-ethyl-D2-1,2,4-triazoline-5-thione) on the central nervous system (CNS) of mice were studied.

Synthesis and some pharmacological properties of 3-(piperidin-4-yl)-4-substituted-D2-1,2,4-triazoline-5-thione derivatives.

Synthesis of 3-(piperidin-4-yl)-4-substituted-D-2-1,2,4-triazoline-5-thione derivatives, AS-1-AS-4 is described. Results of a preliminary pharmacological screening of two compounds AS-1 and AS-3 are presented.

Synthesis and biological activity of new derivatives of 3-(3,4-diaryl-1,2,4-triazole-5-yl)propenoic acid.

New 3-(3,4-diaryl-1,2,4-triazole-5-yl)propenoic acid derivatives (8-14) were synthesized by condensation of N(3)-substituted amidrazones (1-7) with maleic anhydride. Molecular structure of obtained compounds was confirmed by an elemental analysis, IR and (1)H NMR spectra, and the X-ray crystallography for compound 11. The influence of the compound 9 on the central nervous system (CNS) of mice in some behavioural test was examined.

Preliminary evaluation of CNS effects of 6-O-substituted chelidonine derivatives.

Eleven new derivatives of chelidonine I, obtained by functionalization of the alkaloid hydroxyl group, have been tested for CNS activity in mice exhibiting statistically significant effects.

Synthesis and pharmacological properties of sulfur derivatives of indane-1,3-dione.

Synthesis of sulfur derivatives of indane-1,3-dione, VIIb-c, VIIIa-b, IX and X is described. Results of a preliminary pharmacological screening of six compounds [VIIb, VIII, VIIIb, IX, X and XI] are presented.

Synthesis and some pharmacological properties of 3-(4-phenyl-5-oxo-1,2,4-triazolin-1-ylmethyl)-1,2,4-triazolin-5-thione derivatives.

In the reaction of (4-phenyl- or 3,4-diphenyl-5-oxo-1,2,4-triazeolin-1-ylmethyl)-carbohydrazide (IIa, IIb) with isothiocyanates the thiosemicarbazide derivatives [IIIa, b - IXa, b] were obtained. Cyclization of those compounds in the presence of 2% or 10% NaOH led to formation of derivatives with the 1,2,4-triazolin-5-thione system [Xa, b - XV[a, b]. Molecular structure proposed for this group of compounds was confirmed by X-ray structure analysis of Xa and XIVa.