二芳基哌啶类作为 CB1 受体拮抗剂。
Diaryl piperidines as CB1 receptor antagonists.
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2010 Feb 1;20(3):1278-83. doi: 10.1016/j.bmcl.2009.11.075. Epub 2009 Nov 20.
PMID:20018510
Abstract
The syntheses and SAR investigations of novel CB(1) receptor antagonists based on a 1,2-diaryl piperidine core have been described. Optimization of this core afforded a compound with robust in vivo potency by reducing food intake in a mouse DIO model.
摘要
已经描述了基于 1,2-二芳基哌啶核心的新型 CB(1)受体拮抗剂的合成和 SAR 研究。通过降低肥胖小鼠模型中的食物摄入量，对该核心结构进行优化得到了一种具有强大体内活性的化合物。
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