3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl) phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor …

SF Poon, BW Eastman, DF Chapman, J Chung…

文献索引：Poon, Steve F.; Eastman, Brian W.; Chapman, Deborah F.; Chung, Janice; Cramer, Merryl; Holtz, Gregory; Cosford, Nicholas D.P.; Smith, Nicholas D. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 22 p. 5477 - 5480 Title/Abstract Full Text View citing articles Show Details Tehrani, Lida R.; Smith, Nicholas D.; Huang, Dehua; Poon, Steve F.; Roppe, Jeffrey R.; Seiders, Thomas Jon; Chapman, Deborah F.; Chung, Janice; Cramer, Merryl; Cosford, Nicholas D.P. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 22 p. 5061 - 5064

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被引用次数: 25

摘要

Structure–activity relationship studies performed around 3-fluoro-5-(5-pyridin-2-yl-2H- tetrazol-2-yl) benzonitrile for the purpose of developing novel mGlu5 receptor antagonists are described. Synthesis of a series of four-ring tetrazoles led to the discovery of 3-[3-fluoro- 5-(5-pyridin-2-yl-2H-tetrazol-2-yl) phenyl]-4-methylpyridine, a highly potent, brain penetrant, azole-based mGlu5 receptor antagonist.