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ID: ALA4028897
Journal: J Med Chem
Title: Highly Selective Dopamine D3 Receptor Antagonists with Arylated Diazaspiro Alkane Cores.
Authors: Reilly SW, Griffin S, Taylor M, Sahlholm K, Weng CC, Xu K, Jacome DA, Luedtke RR, Mach RH.
Abstract: 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.
CiteXplore: 29125762