Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
Bioorg Med Chem Lett. 2011 Oct 15;21(20):6154-60. doi: 10.1016/j.bmcl.2011.08.034. Epub 2011 Aug 11.
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 1f and the indole 1g display the optimal orientation of the carboxylate for enhanced FXR agonist potency.
为了进一步探索 GW 40641a 的构象限制类似物中酸性部分的最佳位置，我们制备了一系列取代的二苯乙烯衍生物。苯并噻吩 1f 和吲哚 1g 显示出最佳的羧酸盐取向，可增强 FXR 激动剂的效力。
