NR2B-SelectiveN-Methyl-d-aspartate Antagonists: Synthesis and Evaluation of 5-Substituted Benzimidazoles
Journal of Medicinal Chemistry2004Vol. 47(8), pp. 2089–2096
Citations Over TimeTop 21% of 2004 papers
John A. McCauley, Cory R. Theberge, Joseph J. Romano, S.B. Billings, Kenneth D. Anderson, David A. Claremon, Roger Freidinger, Rodney A. Bednar, Scott D. Mosser, Stanley L. Gaul, Thomas Connolly, Cindra Condra, Menghang Xia, Michael E. Cunningham, Bohumil Bednář, Gary L. Stump, Joseph J. Lynch, Alison Macaulay, Keith A. Wafford, Kenneth S. Koblan, Nigel J. Liverton
Abstract
Two classes of 5-substituted benzimidazoles were identified as potent antagonists of the NR2B subtype of the N-methyl-d-aspartate (NMDA) receptor. Selected compounds show very good selectivity versus the NR2A, NR2C, and NR2D subtypes of the NMDA receptor as well as versus hERG-channel activity and alpha(1)-adrenergic binding. Benzimidazole 37a shows excellent activity in the carrageenan-induced mechanical hyperalgesia assay in rats as well as good pharmacokinetic behavior in dogs.
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