2-{2-[3-(Pyridin-3-yloxy) phenyl]-2H-tetrazol-5-yl} pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist

D Huang, SF Poon, DF Chapman, J Chung…

文献索引：Huang, Dehua; Poon, Steve F.; Chapman, Deborah F.; Chung, Janice; Cramer, Merryl; Reger, Thomas S.; Roppe, Jeffrey R.; Tehrani, Lida; Cosford, Nicholas D.P.; Smith, Nicholas D. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 22 p. 5473 - 5476

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被引用次数: 26

摘要

Structure–activity relationship studies on 3-(5-pyridin-2-yl-2H-tetrazol-2-yl) benzonitrile 2 led to the discovery of 2-{2-[3-(pyridin-3-yloxy) phenyl]-2H-tetrazol-5-yl} pyridine (10)—a highly potent and selective mGlu5 receptor antagonist with good brain penetration and in vivo receptor occupancy in rat and cross-species oral bioavailability.