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Synthesis new 1,2,4-triazoline- and 1,3,4-tiadiazole - isoxazole derivatives with immunomodulatory activities |
Marcin Mączyński 1, Michał Zimecki 2, Stanisław Ryng 1 |
1. Wrocław Medical University, Faculty of Pharmacy, Department of Organic Chemistry, Grodzka 9, Wrocław 50-137, Poland |
Abstract |
Intensive studies on new, biologically active isoxazole derivatives, have been conducted for the last few decades. We synthesized a group of monocyclic and bicyclic isoxazole derivatives. In the group of monocyclic compounds, the pharmacophore structure was a fragment of 5-amino-3-methyl-4-isoxazolecarboxylic acid. The importance of the pharmacophore structure of 5-amino-3-methylo-4-isoxazolecarboxylic acid, contained in N'-substituted hydrazides, semicarbazides, semithiocarbazides of that acid with immunosupressory activities and isoxazoleoxadiazol, isoxazolopirazol and isoxazolopirol, with high immunomodulatory activities, was confirmed in several patents. Looking for active immunomodulators we synthesized new 4-substituted 3-(5-amino-3-methyl-4-isoxazole)-1,2,4,-triazoline-5-tione and 5-substituted 2-(5-amino-3-methyl-4-isoxazole)-1,3,4-tiadiazole derivatives. We obtained the compounds in reaction of 5-amino-3-methyl-4-isoxazolecarboxylic acid thiosemicarbazides with conc. sulphuric acid or sodium hydroxide. |
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Presentation: Poster at VI Multidyscyplinarna Konferencja Nauki o Leku, by Marcin MączyńskiSee On-line Journal of VI Multidyscyplinarna Konferencja Nauki o Leku Submitted: 2008-03-12 11:23 Revised: 2009-06-07 00:48 |