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

…, YA Tahirovic, N Kurtkaya, P Mullasseril, H Yuan…

Index: Mosley, Cara A.; Myers, Scott J.; Murray, Ernest E.; Santangelo, Rose; Tahirovic, Yesim A.; Kurtkaya, Natalie; Mullasseril, Praseeda; Yuan, Hongjie; Lyuboslavsky, Polina; Le, Phuong; Wilson, Lawrence J.; Yepes, Manuel; Dingledine, Ray; Traynelis, Stephen F.; Liotta, Dennis C. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 17 p. 6463 - 6480

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Citation Number: 24

Abstract

The synthesis and structure–activity relationship analysis of a novel class of amide-based biaryl NR2B-selective NMDA receptor antagonists are presented. Some of the studied compounds are potent, selective, non-competitive, and voltage-independent antagonists of NR2B-containing NMDA receptors. Like the founding member of this class of antagonists (ifenprodil), several interesting compounds of the series bind to the amino terminal ...