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首页> 外文期刊>Archives of pharmacal research >Synthesis and biological activity of 5-{4-(2-(methyl-p-substituted phenylamino)ethoxy)benzyl}thiazolidine-2,4-diones.
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Synthesis and biological activity of 5-{4-(2-(methyl-p-substituted phenylamino)ethoxy)benzyl}thiazolidine-2,4-diones.

机译:5- {4-(2-(甲基-对-取代的苯基氨基)乙氧基)苄基}噻唑烷-2,4-二酮的合成和生物活性。

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摘要

Thiazolidinedione derivatives are potential antidiabetic drugs that bind and activate peroxisome proliferator activated receptor gamma (PPARgamma), which is a member of the nuclear hormone receptor superfamily and enhances insulin sensitivity. In an effort to develop a novel and effective thiazolidindione derivative, 5-{4-[2-(methyl-p-substituted phenylamino) ethoxy] benzyl} thiazolidine-2,4-diones 7 have been prepared by Mitsunobu reaction of the hydrophobic segment, methyl-p-substituted phenylaminoethanol 4 with hydroxybenzylthiazolidinedione 5 and their ability to activate PPARgamma and inhibit LPS-induced NO production were evaluated.
机译:噻唑烷二酮衍生物是潜在的抗糖尿病药物,其结合并激活过氧化物酶体增殖物激活受体γ(PPARgamma),后者是核激素受体超家族的成员,并增强胰岛素敏感性。为了开发新颖且有效的噻唑烷二酮衍生物,通过疏水链段的Mitsunobu反应制备了5- {4- [2-(甲基-对-取代的苯基氨基)乙氧基]苄基}噻唑烷-2,4-二酮7。评估了具有羟基苄基噻唑烷二酮5的甲基对位取代的苯基氨基乙醇4及其活​​化PPARγ和抑制LPS诱导的NO生成的能力。

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