Structure-activity Relationships in a Novel Series of 7-substituted-aryl Quinolines and 5-substituted-aryl Benzothiazoles at the Metabotropic Glutamate Receptor Subtype 5

Overview

Journal Bioorg Med Chem

Specialties Biochemistry
Chemistry

Date 2010 Apr 13

PMID 20382541

Citations 6

Authors

Peng Zhang

Mu-Fa Zou

Alice L Rodriguez

P Jeffrey Conn

Amy Hauck Newman

Affiliations

Soon will be listed here.

Abstract

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.

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