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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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Autores principales: Paprocka, Renata, Wiese-Szadkowska, Małgorzata, Kołodziej, Przemysław, Kutkowska, Jolanta, Balcerowska, Sara, Bogucka-Kocka, Anna
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10180335/
https://www.ncbi.nlm.nih.gov/pubmed/37175218
http://dx.doi.org/10.3390/molecules28093808
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author Paprocka, Renata
Wiese-Szadkowska, Małgorzata
Kołodziej, Przemysław
Kutkowska, Jolanta
Balcerowska, Sara
Bogucka-Kocka, Anna
author_facet Paprocka, Renata
Wiese-Szadkowska, Małgorzata
Kołodziej, Przemysław
Kutkowska, Jolanta
Balcerowska, Sara
Bogucka-Kocka, Anna
author_sort Paprocka, Renata
collection PubMed
description 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 3a–3g were obtained in reactions of amidrazones 1a–1g with succinic anhydride. Several analyses of proton and carbon nuclear magnetic resonance ((1)H NMR, (13)C NMR, respectively), as well as high-resolution mass spectra (HRMS), confirmed the structures of 1,2,4-triazole derivatives 3a–3g. 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 3a–3g 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 3a–3g were studied against Gram-positive and Gram-negative bacterial strains and Rhabditis sp. culture. Despite the lack of toxicity, compounds 3a–3g significantly reduced the level of TNF-α. Derivatives 3a, 3c and 3e also decreased the release of IFN-γ. Taking all of the results into consideration, compounds 3a, 3c and 3e show the most beneficial anti-inflammatory effects.
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spelling pubmed-101803352023-05-13 Evaluation of Biological Activity of New 1,2,4-Triazole Derivatives Containing Propionic Acid Moiety Paprocka, Renata Wiese-Szadkowska, Małgorzata Kołodziej, Przemysław Kutkowska, Jolanta Balcerowska, Sara Bogucka-Kocka, Anna Molecules Article 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 3a–3g were obtained in reactions of amidrazones 1a–1g with succinic anhydride. Several analyses of proton and carbon nuclear magnetic resonance ((1)H NMR, (13)C NMR, respectively), as well as high-resolution mass spectra (HRMS), confirmed the structures of 1,2,4-triazole derivatives 3a–3g. 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 3a–3g 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 3a–3g were studied against Gram-positive and Gram-negative bacterial strains and Rhabditis sp. culture. Despite the lack of toxicity, compounds 3a–3g significantly reduced the level of TNF-α. Derivatives 3a, 3c and 3e also decreased the release of IFN-γ. Taking all of the results into consideration, compounds 3a, 3c and 3e show the most beneficial anti-inflammatory effects. MDPI 2023-04-29 /pmc/articles/PMC10180335/ /pubmed/37175218 http://dx.doi.org/10.3390/molecules28093808 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Paprocka, Renata
Wiese-Szadkowska, Małgorzata
Kołodziej, Przemysław
Kutkowska, Jolanta
Balcerowska, Sara
Bogucka-Kocka, Anna
Evaluation of Biological Activity of New 1,2,4-Triazole Derivatives Containing Propionic Acid Moiety
title Evaluation of Biological Activity of New 1,2,4-Triazole Derivatives Containing Propionic Acid Moiety
title_full Evaluation of Biological Activity of New 1,2,4-Triazole Derivatives Containing Propionic Acid Moiety
title_fullStr Evaluation of Biological Activity of New 1,2,4-Triazole Derivatives Containing Propionic Acid Moiety
title_full_unstemmed Evaluation of Biological Activity of New 1,2,4-Triazole Derivatives Containing Propionic Acid Moiety
title_short Evaluation of Biological Activity of New 1,2,4-Triazole Derivatives Containing Propionic Acid Moiety
title_sort evaluation of biological activity of new 1,2,4-triazole derivatives containing propionic acid moiety
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10180335/
https://www.ncbi.nlm.nih.gov/pubmed/37175218
http://dx.doi.org/10.3390/molecules28093808
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