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首页> 外文期刊>Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry >Anti-hyperglycemic evaluation of 2,4-thiazolidinedione and rhodanine derivatives
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Anti-hyperglycemic evaluation of 2,4-thiazolidinedione and rhodanine derivatives

机译:2,4-噻唑烷二酮和若丹宁衍生物的抗高血糖评估

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A novel series comprising of 10 derivatives of two chemical entities thiazolidinedione and rhodanine were synthesized and characterized physicochemically as well as by spectral means. The synthesized derivatives (THP, RHP, RHB, MB01-MB09) were then screened for anti-hyperglycemic activity in fructose-induced diabetic animal model. It can be concluded that presence of piperazine and N-methyl piperazine at N-3 of thiazolidinedione and rhodanine derivatives have shown significant activity in comparison to aromatic amine substitution. The presence of ether linkage is the primary requisite for anti-hyperglycemic activity. Condensation of benzylidene with lipophilic moiety i.e. benzothiazole enhanced the activity of the synthesized derivatives. Piperazine substituted compound, MB01was most potent anti-hyperglycemic activity that might be due to the availability of free nitrogen at receptor site.
机译:合成了由两个化学实体的10个衍生物组成的新系列,其中噻唑烷二酮和若丹宁的理化性质以及通过光谱手段进行表征。然后在果糖诱导的糖尿病动物模型中筛选合成的衍生物(THP,RHP,RHB,MB01-MB09)的降血糖活性。可以得出结论,与芳族胺取代相比,噻唑烷二酮和若丹宁衍生物在N-3处存在哌嗪和N-甲基哌嗪已显示出显着的活性。醚键的存在是抗高血糖活性的首要条件。亚苄基与亲脂性部分即苯并噻唑的缩合提高了合成衍生物的活性。哌嗪取代的化合物MB01具有最强的抗高血糖活性,这可能是由于受体位点上的游离氮的有效性所致。

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