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 - were obtained in reactions of amidrazones - with succinic anhydride. Several analyses of proton and carbon nuclear magnetic resonance (H NMR, C NMR, respectively), as well as high-resolution mass spectra (HRMS), confirmed the structures of 1,2,4-triazole derivatives -. 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 - 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 - were studied against Gram-positive and Gram-negative bacterial strains and sp. culture. Despite the lack of toxicity, compounds - significantly reduced the level of TNF-α. Derivatives , and also decreased the release of IFN-γ. Taking all of the results into consideration, compounds , and show the most beneficial anti-inflammatory effects.
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http://dx.doi.org/10.3390/molecules28093808 | DOI Listing |
Mol Divers
August 2016
Bioengineering & Environmental Sciences, CSIR-Indian Institute of Chemical Technology, Hyderabad, India.
A new class of compounds, structurally related to the breast cancer drug tamoxifen, was designed and synthesized. The McMurry coupling reaction was used as the key synthetic step in the preparation of these analogs, and the structural assignments were made on the basis of [Formula: see text] NMR, [Formula: see text] NMR, and HRMS studies. The absolute stereochemistry of E and Z isomers was unambiguously confirmed by a single-crystal X-ray diffraction analysis.
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