Department Chemie und Pharmazie, Pharmazeutische Chemie, Friedrich-Alexander-Universität Erlangen-Nürnberg, Schuhstraße 19, 91052 Erlangen (Germany).
ChemMedChem. 2014 Jan;9(1):151-68. doi: 10.1002/cmdc.201300369. Epub 2013 Nov 21.
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.
为了制备和生物评估 38 种新型潜在的 US28 别构调节剂，我们采用了一种简单的合成路线，涉及自由基芳基化反应。该研究基于以前的先导结构，但将二氢异喹啉酮部分替换为取代的联苯。对联苯衍生配体的新结构-活性关系的研究导致了初步的药效基团模型的发现，并发现了四个具有完全反向激动剂特性的有前途的候选物。
