Synthesis and Biological Evaluation of Biphenyl Amides That Modulate the US28 Receptor
Synthesis and Biological Evaluation of Biphenyl Amides That Modulate the US28 Receptor
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DOI：
10.1002/cmdc.201300369
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发表时间：
2014-01-01
期刊：
影响因子：
3.4
通讯作者：
Heinrich, Markus R.
中科院分区：
文献类型：
--
作者：
Kralj, Ana;Kurt, Elif;Heinrich, Markus R.
为了制备和生物学评价38种新的潜在US 28变构调节剂，我们采用了一种简单的合成路线，包括自由基芳基化。这项研究是基于以前的铅结构，但与二氢异喹啉酮部分取代取代联苯。新的联苯衍生的配体之间的结构-活性关系的调查导致了初步的药效团模型和四个有前途的候选人的发现与完整的反向激动剂性能。
To prepare and biologically evaluate 38 new potential US28 allosteric modulators, we employed a straightforward synthetic route involving radical arylation. The study was based on a former lead structure but with the dihydroisoquinolinone moiety replaced by substituted biphenyls. The investigation of structure-activity relationships among the new biphenyl-derived ligands led to a preliminary pharmacophore model and the discovery of four promising candidates with full inverse agonist properties.