一种新型（R）-4,4-二氟哌啶支架作为多巴胺受体4（DR）拮抗剂的发现、表征及生物学评价
Discovery, characterization and biological evaluation of a novel (R)-4,4-difluoropiperidine scaffold as dopamine receptor 4 (DR) antagonists.
作者信息
Jeffries Daniel E, Witt Jonathan O, McCollum Andrea L, Temple Kayla J, Hurtado Miguel A, Harp Joel M, Blobaum Anna L, Lindsley Craig W, Hopkins Corey R
机构信息
Department of Chemistry, Vanderbilt University, Nashville, TN 37232, United States.
Department of Pharmacology, Vanderbilt University, Nashville, TN 37232, United States; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, TN 37232, United States.
出版信息
Bioorg Med Chem Lett. 2016 Dec 1;26(23):5757-5764. doi: 10.1016/j.bmcl.2016.10.049. Epub 2016 Oct 17.
Herein, we report the synthesis and structure-activity relationship of a novel series of (R)-4,4-difluoropiperidine core scaffold as dopamine receptor 4 (D) antagonists. A series of compounds from this scaffold are highly potent against the D receptor and selective against the other dopamine receptors. In addition, we were able to confirm the active isomer as the (R)-enantiomer via an X-ray crystal structure.
在此，我们报告了一系列新型（R）-4,4-二氟哌啶核心支架作为多巴胺受体4（D4）拮抗剂的合成及构效关系。该支架系列的一系列化合物对D4受体具有高度活性，且对其他多巴胺受体具有选择性。此外，我们通过X射线晶体结构证实了活性异构体为（R）-对映体。
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