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一些新型茶碱衍生物的合成及其降血糖活性

Synthesis and hypoglycemic activity of some new theophylline derivatives.

作者信息

Alafeefy Ahmed M, Alqasoumi Saleh I, Abdel Hamid Sami G, El-Tahir Kamal E H, Mohamed Menshawy, Zain Mohamed E, Awaad Amani S

机构信息

Department of Pharmaceutical Chemistry and.

出版信息

J Enzyme Inhib Med Chem. 2014 Jun;29(3):443-8. doi: 10.3109/14756366.2013.795957. Epub 2013 May 23.

Abstract

Thirty-one new theophylline derivatives have been synthesized and evaluated for their hypoglycemic activity. Compounds 24 (56% reduction) and 31 (57% reduction) showed better hypoglycemic activity than the standard drug glibenclamide which showed 52% reduction in serum glucose level. Compound 27 remarkably reduced serum glucose level by 53%. Ten compounds showed varying degrees of hypoglycemic activity ranging from 20 to 37% reduction in serum glucose level compared to the standard drug. The aromatic amide functionality is the common feature of these theophylline hypoglycemic derivatives. However, anthranilamide and or aliphatic amides proved to be the least active compounds in the present series.

摘要

已合成了31种新的茶碱衍生物,并对其降血糖活性进行了评估。化合物24(血糖降低56%)和31(血糖降低57%)显示出比标准药物格列本脲更好的降血糖活性,格列本脲使血清葡萄糖水平降低了52%。化合物27显著降低血清葡萄糖水平达53%。与标准药物相比,有10种化合物表现出不同程度的降血糖活性,血清葡萄糖水平降低幅度在20%至37%之间。芳香酰胺官能团是这些茶碱降血糖衍生物的共同特征。然而,邻氨基苯甲酰胺和/或脂肪族酰胺被证明是本系列中活性最低的化合物。

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