Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

Andrew S Felts,Alice L Rodriguez,Ryan D Morrison,Anna L Blobaum,Frank W Byers,J Scott Daniels,Colleen M Niswender,P Jeffrey Conn,Craig W Lindsley,Kyle A Emmitte

Bioorganic & Medicinal Chemistry Letters（2018）

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摘要

•New negative allosteric modulators of metabotropic glutamate receptor subtype 5.•Quinoline-8-carboxamides are functional as a picolinamide replacement.•Certain carbon-based linkers are alternatives to an ether linker.

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关键词

Metabotropic glutamate receptor subtype 5 (mGlu5),Negative allosteric modulator (NAM),Central nervous system (CNS),G protein-coupled receptor (GPCR),Quinoline

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