Search for potential hypoglycemic agents among potassium salts of 3-benzyl-8-substituted xanthines

K. Aleksandrova, Yevhen S. Pruhlo, Y. Mykhalchenko, O. Shkoda, O. Y. Cherchesova
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Abstract

Nowadays, the prevalence of metabolic syndrome (MS) is a serious problem among the world’s population. Metabolic syndrome includes the so-called “deadly” quartet – hypertension, type 2 diabetes mellitus (diabetes mellitus), dyslipidemia and alimentary obesity. After all, type 2 diabetes is included in the list of pathologies of the metabolic syndrome, it is important to find ways to alleviate the disease. Derivatives of such a heterocyclic system as xanthine are of great interest in this aspect. The aim of the study was to explore the hypoglycemic activity of newly synthesized water-soluble derivatives of 3-benzyl-8-substituted xanthines. Materials and methods. We obtained water-soluble potassium 3-benzyl-8-R-xanthin-7-ides, the structure and individuality of which were confirmed by a set of physical-chemical studies. Results. The hypoglycemic effect of the newly synthesized compounds was assessed by an oral glucose tolerance test. The obtained data were processed using modern statistical in silico-methods. Conclusions. The results of the hypoglycemic activity study among the potassium salts of 3-benzyl-8-substituted xanthine derivatives showed, that some new compounds are in close vicinity to the reference drug’s hypoglycemic action.  
在3-苄基-8-取代黄嘌呤的钾盐中寻找潜在的降糖剂
目前,代谢综合征(MS)的患病率是世界人口中一个严重的问题。代谢综合征包括所谓的“致命”四重——高血压、2型糖尿病、血脂异常和消化道肥胖。毕竟,2型糖尿病被包括在代谢综合征的病理列表中,找到减轻疾病的方法是很重要的。黄嘌呤这类杂环体系的衍生物在这方面引起了极大的兴趣。研究新合成的3-苄基-8-取代黄嘌呤水溶性衍生物的降糖活性。材料和方法。我们得到了水溶性的3-苄基-8- r-黄素-7-ides,并通过一系列理化研究证实了其结构和特性。通过口服葡萄糖耐量试验评估新合成化合物的降糖作用。所得数据采用现代统计学方法进行处理。对3-苄基-8-取代黄嘌呤衍生物的钾盐的降糖活性研究结果表明,一些新化合物的降糖作用与参比药物非常接近。
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