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.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Amides / chemical synthesis*
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Amides / chemistry*
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Animals
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Binding Sites
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CHO Cells
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Chemistry, Pharmaceutical / methods*
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Cricetinae
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Cricetulus
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Drug Design
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Mice
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Models, Chemical
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Models, Molecular
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Molecular Conformation
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Receptor, Metabotropic Glutamate 5
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Receptors, Metabotropic Glutamate / antagonists & inhibitors*
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Structure-Activity Relationship
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Substance-Related Disorders / drug therapy
Substances
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Amides
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Grm5 protein, mouse
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Receptor, Metabotropic Glutamate 5
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Receptors, Metabotropic Glutamate