Synthesis of potential antiexudative preparations for 2-((4-amino-5-(furan-2-il)-1,2,4-triazole-(4H)-3-yl)-sulfanyl)-N-acetamide series
Journal Title: ScienceRise: Pharmaceutical Science - Year 2019, Vol 0, Issue 3
Abstract
<p><strong>Aim.</strong> Conduct the purposeful synthesis of new potential biologically active substances of derivatives of 2 - ((4-amino-5- (furan-2-yl) -1,2,4-triazol (4H) -3-yl) -sulfanyl) -N-acetamides and evaluate their anti-exudative activity on the model of formalin edema in rats.</p><p><strong>Materials and methods.</strong> In this work, standard methods of organic synthesis, physical and chemical methods of proofing the structure of synthesized compounds, elemental analysis, <sup>1</sup>H NMR spectroscopy, chromatographic mass spectrometry, and antiexudative activity were studied on the model of formalin edema in rats using a digital plethysmometer.</p><p><strong>Results.</strong> By alkylation of 2-((4-amino-5-(furan-2-yl))-4H-1,2,4-triazole-3-thione with N-aryl-substituted α-chloroacetamides in ethanol in an alkaline medium, (4-amino-5-(furan-2-yl)-1,2,4-triazole(4H)-3-yl)-sulfanyl)-N-acetamide. After crystallization we obtained white or light yellow crystalline substances with clear melting temperatures. On the model of formalin edema in rats, the antiexudative activity of the newly synthesized 2-((4-amino-5-(furan-2-yl)-1,2,4-triazole (4H) -3-yl) -sulfanil)-N-acetamides was studied. According to the results of the research, a dependence between "chemical structure – antiexudative activity" of the first synthesized compounds was established. The results of experimental studies showed that fifteen out of twenty one compounds showed anti-exudative activity, eight of which exceeded this activity or were at the reference level of sodium diclofenac.</p><p><strong>Conclusions. </strong>Synthesis of twenty one compounds of 2-((4-amino-5- (furan-2-yl)-1,2,4-triazole(4H)-3-yl)-sulfanyl)-N-acetamide derivatives was carried out and an evaluation of antiexudative activity, the dependence "chemical structure - antiexudative activity" was established. Leading compounds for antiexudative activity were found</p>
Authors and Affiliations
Natalia Chalenko, Anatoly Demchenko, Ganna Syrova
Keywords
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- EP ID EP647848
- DOI 10.15587/2519-4852.2019.171878
- Views 122
- Downloads 0
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