新型[1-(4-羟基苄基)-1H-吲哚-5-氧基]乙酸化合物系列的设计与合成：强效、选择性甲状腺激素受体β激动剂
Design and synthesis of a novel series of [1-(4-hydroxy-benzyl)-1H-indol-5-yloxy]-acetic acid compounds as potent, selective, thyroid hormone receptor β agonists.
作者信息
Burkholder Timothy P, Cunningham Brian E, Clayton Joshua R, Lander Peter A, Brown Matthew L, Doti Robert A, Durst Gregory L, Montrose-Rafizadeh Chahrzad, King Constance, Osborne Harold E, Amos Robert M, Zink Richard W, Stramm Lawrence E, Burris Thomas P, Cardona Guemalli, Konkol Debra L, Reidy Charles, Christe Michael E, Genin Michael J
机构信息
Discovery Chemistry Research and Technology, Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
Lead Optimization Biology, Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
出版信息
Bioorg Med Chem Lett. 2015 Apr 1;25(7):1377-80. doi: 10.1016/j.bmcl.2015.02.062. Epub 2015 Mar 3.
The design, synthesis, and structure activity relationships for a novel series of indoles as potent, selective, thyroid hormone receptor β (TRβ) agonists is described. Compounds with >50× binding selectivity for TRβ over TRα were generated and evaluation of compound 1c from this series in a model of dyslipidemia demonstrated positive effects on plasma lipid endpoints in vivo.
本文描述了一系列新型吲哚类化合物作为强效、选择性甲状腺激素受体β（TRβ）激动剂的设计、合成及其构效关系。我们制备了对TRβ的结合选择性比对TRα高50倍以上的化合物，并在血脂异常模型中对该系列化合物1c进行评估，结果表明其对体内血浆脂质指标具有积极影响。
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