Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists

Peter C Chua; Johnny Y Nagasawa; Leo S Bleicher; Benito Munoz; Edwin J Schweiger; Lida Tehrani; Jeffrey J Anderson; Merryl Cramer; Janice Chung; Mitchell D Green; Chris D King; Grace Reyes-Manalo; Nicholas D P Cosford

doi:10.1016/j.bmcl.2005.06.099

Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4589-93. doi: 10.1016/j.bmcl.2005.06.099.

Authors

Peter C Chua¹, Johnny Y Nagasawa, Leo S Bleicher, Benito Munoz, Edwin J Schweiger, Lida Tehrani, Jeffrey J Anderson, Merryl Cramer, Janice Chung, Mitchell D Green, Chris D King, Grace Reyes-Manalo, Nicholas D P Cosford

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2 3535 General Atomics Court, San Diego, CA 92121, USA. [email protected]

PMID: 16115767
DOI: 10.1016/j.bmcl.2005.06.099

Abstract

Structure-activity relationship studies leading to the discovery of novel mGlu5 receptor antagonists are described. These compounds show high in vitro potency, have good in vivo receptor occupancy, and a reasonable intravenous pharmacokinetic profile.

MeSH terms

Excitatory Amino Acid Antagonists / pharmacokinetics
Excitatory Amino Acid Antagonists / pharmacology*
Pyridines / pharmacokinetics
Pyridines / pharmacology*
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate / antagonists & inhibitors*

Substances

Excitatory Amino Acid Antagonists
Pyridines
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate