Institute of Organic Chemistry, RWTH Aachen University, Landoltweg 1, D-52056 Aachen, Germany.
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4888-90. doi: 10.1016/j.bmcl.2011.06.029. Epub 2011 Jun 22.
The syntheses and biological profiles of sulfoximine-based Vioxx analogs 2 are described. Interesting data have been obtained for 2a, which shows a selective COX-2 inhibition (albeit not as strong as Vioxx itself) exhibiting reduced hERG activity compare to the parent sulfone Vioxx (1).
基于磺酰亚胺的万络类似物 2 的合成和生物特性描述如下。 2a 获得了有趣的数据,其表现出选择性 COX-2 抑制作用(尽管不如万络本身强),与母体砜万络(1)相比,hERG 活性降低。