Chemical properties of amino- and thio-derivatives of 1,2,4-triazoles
Aim. A number of references of the last ten years have been carefully studied with bibliosemantic method to compile information on the participation of 1,2,4-triazoles in chemical reactions. Introduction of new domestic drugs intopractice, which could compete with expensive imported drugs,is oneof t...
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Zaporozhye State Medical University,
2015-04-01T00:00:00Z.
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| Summary: | Aim. A number of references of the last ten years have been carefully studied with bibliosemantic method to compile information on the participation of 1,2,4-triazoles in chemical reactions. Introduction of new domestic drugs intopractice, which could compete with expensive imported drugs,is oneof the most important social and economic problem sof the pharmaceutical industry. The key step in the creation of original drugs is a purposeful synthesis of biologically active substances with pronounced pharmacological effect and low toxicity. Results. It has been established that the presence of amino and thiol groups provides high reactivity of the starting compounds. It is known that 1,2,4-triazole nucleus is a structural fragment of many synthetic drugs with antifungal (fluconazole, intrakonazol), antidepressant (trazodone, alprazolam), antiviral (thiotriazolin), wound healing and hepatoprotective activity. That's why the 4-amino and 3-thio-1,2,4-triazoles have attracted our attention as potential biologically active compounds which can become the basis of future drugs. Quite powerful material has been gained in the last decade in terms of chemical reactions with the participation of 4-amino and 3-thio-1,2,4-triazoles. This is due to the fact that 1,2,4-triazoles are used not only to create drugs, but also for the manufacture of various products, which are widely used in agriculture, industry, etc. But there are no well-known information in recent years that could generalize chemical conversion with the participation of amino- and thio- derivatives of 1,2,4-triazoles. That is why this purpose became the main goal of our work. Condensation reaction with aromatic aldehydes in a series of 4-amino-3-thio-1,2,4-triazoles has been studied. The article presents data on the analysis further change with above named substances, their participation in cyclization reactions, condensation of aromatic aldehydes, interaction with halogen carbonyl compounds with aryl nitriles of carboxylic acids and conversation 1,2,4-triazole-3-thioacetic acids in sulfoaceticacids and ester receiving, salts and hydrazides to broaden the search range of pharmacologically active substances. The structure of the synthesized compounds as example 5-(4-dimethylaminobenzylidene)-2-methylthiazol(3,2-b)-1,2,4-triazole-6-one has been confirmed with X-ray examination. Conclusion. It indicates the possibility of expanding spectrum of biological actions and further recommendations of most active compound for enhanced pharmacological studies. |
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| Item Description: | 10.14739/2409-2932.2015.1.41702 2306-8094 2409-2932 |