| Summary: | Parasitic diseases, caused by intestinal helminths, remain a very serious problem in both human and veterinary medicine. While searching for new nematicides we examined a series of 1,2,4-triazole derivatives <b>9</b>–<b>22,</b> obtained during reactions of <i>N</i><sup>3</sup>-substituted amidrazones with itaconic anhydride. Two groups of compounds, <b>9</b>–<b>16</b> and <b>17</b>–<b>22,</b> differed in the position of the double bond on the methacrylic acid moiety. The toxicity of derivatives <b>9</b>–<b>22</b> and the anti-inflammatory activity of <b>12</b> and <b>19</b>–<b>22</b> were studied on peripheral blood mononuclear cells (PBMC). Antiproliferative activity of compounds <b>12</b> and <b>19</b>–<b>22</b> was tested cytometrically in PBMC cultures stimulated by phytohemagglutinin. The influence of derivatives <b>12</b> and <b>19</b>–<b>22</b> on the TNF-α, IL-6, IL-10 and IFN-γ production was determined by ELISA in lipopolysaccharide-stimulated PBMC cultures. Anthelmintic activity of compounds <b>10</b>–<b>22</b> was studied in the <i>Rhabditis</i> sp. nematodes model. Most compounds (<b>11</b>–<b>22</b>) proved to be non-toxic to human PBMC. Derivatives <b>19</b>–<b>22</b> showed anti-inflammatory activity by inhibiting the proliferation of lymphocytes. Moreover, compounds <b>12</b> and <b>19</b>–<b>22</b> significantly reduced the production of TNF-α and derivatives <b>19</b>–<b>21</b> decreased the level of INF-γ. The strongest anti-inflammatory activity was observed for compound <b>21</b>. Compounds <b>12</b> and <b>14</b> demonstrated anthelmintic activity higher than albendazole and may become promising candidates for anthelmintic drugs.
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