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. 2016 Dec 1;26(23):5757-5764.
doi: 10.1016/j.bmcl.2016.10.049. Epub 2016 Oct 17.

Discovery, characterization and biological evaluation of a novel (R)-4,4-difluoropiperidine scaffold as dopamine receptor 4 (D4R) antagonists

Daniel E Jeffries  1 , Jonathan O Witt  1 , Andrea L McCollum  1 , Kayla J Temple  2 , Miguel A Hurtado  3 , Joel M Harp  4 , Anna L Blobaum  2 , Craig W Lindsley  5 , Corey R Hopkins  6
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Discovery, characterization and biological evaluation of a novel (R)-4,4-difluoropiperidine scaffold as dopamine receptor 4 (D4R) antagonists

Daniel E Jeffries et al. Bioorg Med Chem Lett. .

Abstract

Herein, we report the synthesis and structure-activity relationship of a novel series of (R)-4,4-difluoropiperidine core scaffold as dopamine receptor 4 (D4) antagonists. A series of compounds from this scaffold are highly potent against the D4 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.

Keywords: Addiction; Difluoropiperidine; Dopamine 4 receptor; PD-LIDs; Selectivity.

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