Bioorganic and Medicinal Chemistry Letters p. 5473 - 5476 (2004)
Update date:2022-09-26
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.
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. 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.
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