Highly Selective Dopamine D3 Receptor Antagonists with Arylated Diazaspiro Alkane Cores

Sean W. Reilly, Suzy Griffin, Michelle Taylor, Kristoffer Sahlholm, Chi Chang Weng, Kuiying Xu, Daniel A. Jacome, Robert R. Luedtke, Robert H. Mach

Research output: Contribution to journalArticlepeer-review

12 Scopus citations


A series of potent and selective D3 receptor (D3R) analogues with diazaspiro alkane cores were synthesized. Radioligand binding of compounds 11, 14, 15a, and 15c revealed favorable D3R affinity (Ki = 12-25.6 nM) and were highly selective for D3R vs D3R (ranging from 264- to 905-fold). Variation of these novel ligand architectures can be achieved using our previously reported 10-20 min benchtop C-N cross-coupling methodology, affording a broad range of arylated diazaspiro precursors.

Original languageEnglish
Pages (from-to)9905-9910
Number of pages6
JournalJournal of Medicinal Chemistry
Issue number23
StatePublished - 14 Dec 2017


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