Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, United Kingdom.
Bioorg Med Chem Lett. 2010 Dec 1;20(23):7116-9. doi: 10.1016/j.bmcl.2010.09.062. Epub 2010 Sep 17.
A series of novel AMPA receptor positive modulators displaying CNS penetration have been discovered with sub-micromolar activity and good selectivity over the cardiac channel receptor, hERG. We describe here the synthesis of these compounds which are biaryl pyrrolidine and tetrahydrofuran sulfonamides and disclose their activities against the human GluA2 flip isoform homotetrameric receptor.
我们发现了一系列具有新型 AMPA 受体正变构调节剂活性的化合物，这些化合物具有亚微米级的活性和对心脏通道受体 hERG 的良好选择性。我们在这里描述了这些化合物的合成，它们是联苯吡咯烷和四氢呋喃磺酰胺，并披露了它们对人 GluA2 翻转同工型同源四聚体受体的活性。
