Conformationally constrained farnesoid X receptor (FXR) agonists: Alternative replacements of the stilbene
Conformationally constrained farnesoid X receptor (FXR) agonists: Alternative replacements of the stilbene
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DOI：
10.1016/j.bmcl.2011.08.034
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发表时间：
2011-10-15
影响因子：
2.7
通讯作者：
Wisely, Bruce
中科院分区：
文献类型：
--
作者：
Akwabi-Ameyaw, Adwoa;Caravella, Justin A.;Wisely, Bruce
为了进一步探索 GW 4064 1a 构象受限类似物中酸部分的最佳位置，制备了一系列二苯乙烯替代物。苯并噻吩 If 和吲哚 1g 显示了羧酸盐的最佳方向，可增强 FXR 激动剂的效力。 (C) 2011 Elsevier Ltd. 保留所有权利。
To further explore the optimum placement of the acid moiety in conformationally constrained analogs of GW 4064 1a, a series of stilbene replacements were prepared. The benzothiophene If and the indole 1g display the optimal orientation of the carboxylate for enhanced FXR agonist potency. (C) 2011 Elsevier Ltd. All rights reserved.