Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists

新型杂双芳基酰胺类化合物的设计与合成及其作为代谢型谷氨酸受体5亚型拮抗剂的应用

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Abstract

A series of heterobiaryl amides was designed and synthesized as novel mGluR5 antagonists. The synthesis using palladium catalyzed Suzuki-Miyaura cross-coupling reactions provided an array of compounds with a range of in vitro activities. In particular, compound 9e, 4(3,5-difluorophenyl)-N-(6-methylpyridin-1-yl)picolinamide, exhibited nanomolar affinity at the mGluR5 and will serve as a template for future drug design.

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