Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists

Kevin T Nguyen; Christopher F Claiborne; John A McCauley; Brian E Libby; David A Claremon; Rodney A Bednar; Scott D Mosser; Stanley L Gaul; Thomas M Connolly; Cindra L Condra; Bohumil Bednar; Gary L Stump; Joseph J Lynch; Kenneth S Koblan; Nigel J Liverton

doi:10.1016/j.bmcl.2007.04.084

Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3997-4000. doi: 10.1016/j.bmcl.2007.04.084. Epub 2007 Apr 29.

Authors

Kevin T Nguyen¹, Christopher F Claiborne, John A McCauley, Brian E Libby, David A Claremon, Rodney A Bednar, Scott D Mosser, Stanley L Gaul, Thomas M Connolly, Cindra L Condra, Bohumil Bednar, Gary L Stump, Joseph J Lynch, Kenneth S Koblan, Nigel J Liverton

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. kevin_nguyen@merck.com

PMID: 17498948
DOI: 10.1016/j.bmcl.2007.04.084

Abstract

A novel series of cyclic benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity. Compound 29 is orally active in a carrageenan-induced rat hyperalgesia model of pain.

MeSH terms

Administration, Oral
Animals
Benzamidines / administration & dosage
Benzamidines / pharmacology*
Benzamidines / therapeutic use
Excitatory Amino Acid Antagonists / administration & dosage
Excitatory Amino Acid Antagonists / pharmacology*
Models, Biological
Pain / drug therapy
Rats
Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*

Substances

Benzamidines
Excitatory Amino Acid Antagonists
Receptors, N-Methyl-D-Aspartate