Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists

Paul Galatsis; Koji Yamagata; John A Wendt; Cleo J Connolly; John W Mickelson; Jared B J Milbank; Susan E Bove; Christopher S Knauer; Rachel M Brooker; Corinne E Augelli-Szafran; Roy D Schwarz; Jack J Kinsora; Kenneth S Kilgore

doi:10.1016/j.bmcl.2007.09.083

Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8. doi: 10.1016/j.bmcl.2007.09.083. Epub 2007 Sep 29.

Authors

Paul Galatsis¹, Koji Yamagata, John A Wendt, Cleo J Connolly, John W Mickelson, Jared B J Milbank, Susan E Bove, Christopher S Knauer, Rachel M Brooker, Corinne E Augelli-Szafran, Roy D Schwarz, Jack J Kinsora, Kenneth S Kilgore

Affiliation

¹ Department of Medicinal Chemistry, Pfizer Global Research & Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA.

PMID: 17936624
DOI: 10.1016/j.bmcl.2007.09.083

Abstract

We describe three novel regioisomeric series of aryl naphthyridine analogs, which are potent antagonists of the Class III GPCR mGlu5 receptor. The synthesis and in vitro and in vivo pharmacological activities of these analogs are discussed.

Publication types

Comparative Study

MeSH terms

Animals
CHO Cells
Cricetinae
Cricetulus
Naphthyridines / chemical synthesis*
Naphthyridines / pharmacology*
Rats
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate / antagonists & inhibitors*
Receptors, Metabotropic Glutamate / physiology
Stereoisomerism
Structure-Activity Relationship

Substances

Naphthyridines
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate