新型吡唑噻唑烷杂化结构的合成及降糖活性评价

N. Panasenko, M. Bratenko, V. Zvarych, M. Stasevych, M. Vovk
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引用次数: 1

摘要

在温和反应条件下,利用3-芳基-4甲酰基吡唑硫代氨基脲和二乙基乙酰二羧酸酯进行环缩合反应,得到了在功能化吡唑和噻唑烷环之间含有亚甲基腙连接体的新型吡唑噻唑杂化结构。提出了以乙酸为催化剂合成环境双中心硫代氨基脲,作为进一步形成噻唑烷循环的试剂。通过口服合成衍生物对大鼠体内血糖水平的研究,发现所得到的吡唑噻唑烷类化合物具有降糖活性
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Synthesis and Evaluation of Hypoglycemic Activity of New Pyrazolothiazolidine Hybrid Structures
New promising pyrazolothiazolidine hybrid structures, containing a methylenehydrazone linker between functionalized pyrazole and thiazolidine cycles, have been obtained using cyclocondensation of 3-aryl-4formylpyrazole thiosemicarbazones and diethyl acetylenedicarboxylate in mild reactional conditions. The acetic acid was proposed as a catalytic agent for the synthesis of ambident bi-center thiosemicarbazones as reagents for further formation of the thiazolidine cycle. The obtained pyrazolothiazolidines were found to exhibit hypoglycemic activity by in vivo study of glucose level in the blood of rats after oral administration of synthesized derivatives
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