Wang Yonghui, Busch-Petersen Jakob, Wang Feng, Kiesow Terence J, Graybill Todd L, Jin Jian, Yang Zheng, Foley James J, Hunsberger Gerald E, Schmidt Dulcie B, Sarau Henry M, Capper-Spudich Elizabeth A, Wu Zining, Fisher Laura S, McQueney Michael S, Rivero Ralph A, Widdowson Katherine L
Center of Excellence for Drug Discovery, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA.
Bioorg Med Chem Lett. 2009 Jan 1;19(1):114-8. doi: 10.1016/j.bmcl.2008.11.008. Epub 2008 Nov 6.
A series of N-arylpiperazine camphor sulfonamides was discovered as novel CXCR3 antagonists. The synthesis, structure-activity relationships, and optimization of the initial hit that resulted in the identification of potent and selective CXCR3 antagonists are described.
发现了一系列N-芳基哌嗪樟脑磺酰胺作为新型CXCR3拮抗剂。描述了导致鉴定出强效和选择性CXCR3拮抗剂的初始活性化合物的合成、构效关系及优化过程。
