Evaluation of Biological Activity of New 1,2,4-Triazole Derivatives Containing Propionic Acid Moiety

To this day, the quest to find new drugs is still a challenge due to the growing demands of patients suffering from chronic inflammatory diseases and the need for the individualization of therapy. The aim of this research was to synthesize new 1,2,4-triazole derivatives containing propanoic acid moi...

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Bibliographic Details
Main Authors: Renata Paprocka, Małgorzata Wiese-Szadkowska, Przemysław Kołodziej, Jolanta Kutkowska, Sara Balcerowska, Anna Bogucka-Kocka
Format: Article
Language:English
Published: MDPI AG 2023-04-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/28/9/3808
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Summary:To this day, the quest to find new drugs is still a challenge due to the growing demands of patients suffering from chronic inflammatory diseases and the need for the individualization of therapy. The aim of this research was to synthesize new 1,2,4-triazole derivatives containing propanoic acid moiety and to investigate their anti-inflammatory, antibacterial and anthelmintic activity. Compounds <b>3a</b>–<b>3g</b> were obtained in reactions of amidrazones <b>1a</b>–<b>1g</b> with succinic anhydride. Several analyses of proton and carbon nuclear magnetic resonance (<sup>1</sup>H NMR, <sup>13</sup>C NMR, respectively), as well as high-resolution mass spectra (HRMS), confirmed the structures of 1,2,4-triazole derivatives <b>3a</b>–<b>3g</b>. Toxicity, antiproliferative activity and influence on cytokine release (TNF-α: Tumor Necrosis Factor-α, IL-6: Interleukin-6, IFN-γ: Interferon-γ, and IL-10: Interleukin-10) of the compounds <b>3a</b>–<b>3g</b> were evaluated in peripheral blood mononuclear cells culture. Moreover, mitogen-stimulated cell culture was used for biological activity tests. The antimicrobial and anthelmintic activity of derivatives <b>3a</b>–<b>3g</b> were studied against Gram-positive and Gram-negative bacterial strains and <i>Rhabditis</i> sp. culture. Despite the lack of toxicity, compounds <b>3a</b>–<b>3g</b> significantly reduced the level of TNF-α. Derivatives <b>3a</b>, <b>3c</b> and <b>3e</b> also decreased the release of IFN-γ. Taking all of the results into consideration, compounds <b>3a</b>, <b>3c</b> and <b>3e</b> show the most beneficial anti-inflammatory effects.
ISSN:1420-3049