Synthesis, structural activity-relationships, and biological evaluation of novel amide-based allosteric binding site antagonists in NR1A/NR2B N-methyl-d-aspartate receptors

Cara A. Mosley,Scott J. Myers,Ernest E. Murray,Rose Santangelo,Yesim A. Tahirovic,Natalie Kurtkaya,Praseeda Mullasseril,Hongjie Yuan,Polina Lyuboslavsky,Phuong Le,Lawrence J. Wilson,Manuel Yepes,Ray Dingledine,Stephen F. Traynelis,Dennis C. Liotta

Bioorganic & Medicinal Chemistry（2009）

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摘要

The synthesis and biological activity of a novel series of amide-based NR2B-selective NMDA receptor antagonists is detailed. The compounds herein represent a family of compounds with excellent on-target potency and decreased off-target effects when compared with previously described antagonists.

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关键词

NMDA,GluN2B,NR2B-selective antagonists,Neuroprotection

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