Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.

Zhang P, Zou MF, Rodriguez AL, Conn PJ, Newman AH
Bioorg Med Chem. 2010 18 (9): 3026-35

PMID: 20382541 · PMCID: PMC2871681 · DOI:10.1016/j.bmc.2010.03.053

The metabotropic glutamate receptor subtype 5 (mGluR5) has been implicated in numerous neuropsychiatric disorders including addiction. We have discovered that the rigid diaryl alkyne template, derived from the potent and selective noncompetitive mGluR5 antagonist 2-methyl-6-(phenylethynyl)pyridine (MPEP), can serve to guide the design of novel quinoline analogues and pharmacophore optimization has resulted in potent mGluR5 noncompetitive antagonists (EC(50) range 60-100 nM) in the quinoline series.

(c) 2010. Published by Elsevier Ltd.

MeSH Terms (14)

Animals Benzothiazoles Brain Cell Line Drug Design Excitatory Amino Acid Antagonists Inhibitory Concentration 50 Molecular Structure Pyridines Quinolines Rats Receptor, Metabotropic Glutamate 5 Receptors, Metabotropic Glutamate Structure-Activity Relationship

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