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Highly Selective Dopamine D<sub>3</sub> Receptor Antagonists with Arylated Diazaspiro Alkane Cores

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NIAID Data Ecosystem2026-03-10 收录
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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.

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2017-11-21
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