利用高通量合成发现促黑素聚集激素受体R1拮抗剂。
Discovery of melanin-concentrating hormone receptor R1 antagonists using high-throughput synthesis.
作者信息
Su Jing, McKittrick Brian A, Tang Haiqun, Czarniecki Michael, Greenlee William J, Hawes Brian E, O'Neill Kim
机构信息
Department of Chemical Research, Schering-Plough Research Institute K15 2545, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem. 2005 Mar 1;13(5):1829-36. doi: 10.1016/j.bmc.2004.11.046.
A structure-activity study on benzylpiperidine 1 was accomplished by utilizing high-throughput synthesis. Three focused libraries were designed and synthesized to quickly develop SAR. Further optimization led to the discovery of compound 2, an MCH receptor R1 antagonist with over 400-fold improvement in biological activity over the original lead.
通过高通量合成完成了对苄基哌啶1的构效关系研究。设计并合成了三个聚焦文库以快速开发构效关系。进一步优化导致发现了化合物2，一种MCH受体R1拮抗剂，其生物活性比原始先导化合物提高了400多倍。
Zotero 插件