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

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.

SUBMITTER: Kulkarni SS

PROVIDER: S-EPMC1924965 | biostudies-literature | 2007 Apr

REPOSITORIES: biostudies-literature

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

Kulkarni Santosh S SS Newman Amy Hauck AH

Bioorganic & medicinal chemistry letters 20070104 7

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. ...[more]

PMID: 17336520

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