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来自N1-烟酰基-2-吡唑啉-5-酮衍生物及其N1-(氧代烟酰基)类似物的潜在活性降血糖剂。

Potentially active hypoglycemic agents from N1-nicotinoyl-2-pyrazolin-5-one derivatives and their N1-(oxynicotinoyl) analogues.

作者信息

Girges M M, Hanna M A, Rasala D, Berghot M

机构信息

Chemistry Department, Mansoura, Faculty of Science, Mansoura University, Egypt.

出版信息

Arzneimittelforschung. 1992 Nov;42(11):1350-3.

PMID:1492850
Abstract

Several ethyl 2,3-dioxohexanoate 2-arylhydrazone derivatives were obtained via coupling of the appropriate diazonium chlorides with ethyl butanoylacetate. Acetic acid-mediated cyclization of these products with N1-nicotinoyl and/or N1-(oxynicotinoyl)hydrazine derivatives gave a new series of 4-arylhydrazono-3-(n-propyl)-N1-nicotinoyl-2-pyrazolin-5-one s (Va-h) as well as their N1-(oxynicotinoyl) analogues (VIa-h). The structure of the prepared compounds was confirmed on the basis of elemental and spectral data. The hypoglycemic effect, antibacterial activity and toxicity of these agents were evaluated and discussed.

摘要

通过适当的氯化重氮盐与丁酰乙酸乙酯偶联,得到了几种2,3-二氧代己酸乙酯2-芳基腙衍生物。这些产物与N1-烟酰基和/或N1-(氧基烟酰基)肼衍生物在乙酸介导下环化,得到了一系列新的4-芳基腙基-3-(正丙基)-N1-烟酰基-2-吡唑啉-5-酮(Va-h)及其N1-(氧基烟酰基)类似物(VIa-h)。根据元素和光谱数据确定了所制备化合物的结构。对这些药物的降血糖作用、抗菌活性和毒性进行了评估和讨论。

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