Bioorganic & medicinal chemistry letters

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

SS Kulkarni, AH Newman

Index: Kulkarni, Santosh S.; Newman, Amy Hauck Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 7 p. 2074 - 2079

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Citation Number: 21

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.