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- W3139915459 abstract "瞄准:作为新奇 peroxisome 描绘 rhodanine 衍生物的在试管内简历活动 激活proliferator 的受体( PPAR )鲸鱼群妈调节的人基于一个多样的合成复合图书馆的在高产量的屏蔽期间识别的成功( SH00012671 )( HTS )，并且 preliminarily 阐明 PPAR 鲸鱼群妈 agonists.Methods 的这个班的结构活动关系:全身的 PPAR 鲸鱼群妈和视网膜样的 X 受体高山哈( RXR 高山哈)， biotinylated PPAR 反应元素( PPRE )，[~ 3H ] BRL49653 ( rosiglitazone )，并且streptavidin涂的 FlashPlate 或微祷告被用来基于 technology.A recombinant PPRE 向量是的焕发最近试金(矿泉)测量各种各样的混合物的受体绑定性质短暂地与 PPAR 鲸鱼群妈和 RXR 高山一起的 cotransfected 哈进非洲的绿色的原生质标志胡闹肾( CV-1 )房间，并且抄写上的 BRL49653 和测试混合物的效果由 PPAR 鲸鱼群调停了妈被检验酶(记者)决定 responses.3T3-L1 房间被采用决定混合物是否在 PPAR 鲸鱼群妈 activation.Results 之上便于脂肪形成:与 SPA 方法屏蔽的 16 000 件样品，仅仅 1 混合物( SH00012671 )作为 BRL49653 显示了一种类似的有约束力的亲密关系( K_i=186.7 nmol/L )到 PPAR 鲸鱼群妈，但是衍生物基于 SH00012671 的核心结构被综合，他们中的 8 个在 cotransfection 和 pre-adipocyte 区别试金显示出收缩筋活动，在 rhodanine 的基于房间的 assays.A 系列是不活跃的。减少内在的 cytotoxicities， rhodanine 上的硫被改变到氧。当修改类似物通常在基于房间的试金维持了收缩筋功效时，这改变在受体绑定亲密关系导致了减少。学习的类似物，化合物 31 展出了大约70%功效在 cotransfection 和 pre-adipocyte 区别 assays.Conclusion 由 BRL49653 施加了:通过核心上的次要的化学修正，起始的 HTS 的结构撞击了， SH00012671 被转变拥有两个分子( PPAR 鲸鱼群妈绑定)并且细胞(脂肪形成)这里报导的 activities.The rhodanine 衍生物可以在�" @default.
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- W3139915459 title "Rhodanine derivatives as novel peroxisome proliferator-activated recep- tor Y agonists" @default.
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