具有哌嗪基 - 哌啶核心的新型CXCR3拮抗剂。
Novel CXCR3 antagonists with a piperazinyl-piperidine core.
作者信息
McGuinness Brian F, Carroll Carolyn DiIanni, Zawacki Lisa Guise, Dong Guizhen, Yang Cangming, Hobbs Doug W, Jacob-Samuel Biji, Hall James W, Jenh Chung-Her, Kozlowski Joseph A, Anilkumar Gopinadhan N, Rosenblum Stuart B
机构信息
Ligand Pharmaceuticals, 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA.
出版信息
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5205-8. doi: 10.1016/j.bmcl.2009.07.020. Epub 2009 Jul 9.
High-throughput screening of an encoded combinatorial aryl piperazine library led to the identification of a novel series of potent piperazinyl-piperidine based CXCR3 antagonists. Analogs of the initial hit were synthesized via solid and solution phase methods to probe the influence of structure on the CXCR3 binding of these molecules. Various functional groups were found to contribute to the overall potency and essential molecular features were identified.
对一个编码组合芳基哌嗪文库进行高通量筛选，从而鉴定出一系列基于哌嗪基哌啶的新型强效CXCR3拮抗剂。通过固相和溶液相方法合成了最初活性化合物的类似物，以探究结构对这些分子与CXCR3结合的影响。发现各种官能团对整体效力有贡献，并确定了关键的分子特征。
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