CCR4拮抗剂的优化：侧链探索
Optimization of CCR4 antagonists: side-chain exploration.
作者信息
Purandare Ashok V, Wan Honghe, Gao Aiming, Somerville John, Burke Christine, Vaccaro Wayne, Yang Xiaoxia, McIntyre Kim W, Poss Michael A
机构信息
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA.
出版信息
Bioorg Med Chem Lett. 2006 Jan 1;16(1):204-7. doi: 10.1016/j.bmcl.2005.09.022. Epub 2005 Oct 19.
PMID:16236499
Abstract
The design, synthesis, and activity of novel and selective small molecule antagonists of the CC chemokine receptor-4 (CCR4) are presented. Compound 8c was efficacious in a murine allergic inflammation model (ED(50) 30 mg/kg).
摘要
本文介绍了新型选择性CC趋化因子受体4（CCR4）小分子拮抗剂的设计、合成及活性。化合物8c在小鼠过敏性炎症模型中有效（半数有效剂量为30mg/kg）。
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