Merck Serono SA, Geneva, Switzerland.
Bioorg Med Chem Lett. 2010 Jun 15;20(12):3614-7. doi: 10.1016/j.bmcl.2010.04.113. Epub 2010 Apr 28.
The discovery of a novel series of CXCR3 antagonists is described. Starting from an HTS positive, iterative optimization gave potent compounds (IC(50) 15 nM in a chemotaxis assay). The strategy employed to improve the metabolic stability of these derivatives is described.
本文描述了一类新型 CXCR3 拮抗剂的发现。从高通量筛选得到阳性结果开始，经过反复优化得到了活性很强的化合物（在趋化实验中的 IC50 为 15 nM）。本文还介绍了提高这类衍生物代谢稳定性所采用的策略。
