The Experts below are selected from a list of 360 Experts worldwide ranked by ideXlab platform
Nicholas D Smith - One of the best experts on this subject based on the ideXlab platform.
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3 substituted 5 5 pyridin 2 yl 2h tetrazol 2 yl benzonitriles identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Lida R Tehrani, Steve F Poon, Deborah F Chapman, Janice Chung, Merryl Cramer, Nicholas D Smith, Dehua Huang, Jeffrey Roger Roppe, Thomas Jon Seiders, Nicholas D P CosfordAbstract:Structure-activity relationship studies on the phenyl ring of 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile 2 led to the discovery that small, non-hydrogen bond donor substituents at the 3-position led to a substantial increase in in vitro potency. In particular, 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile (7) is a highly potent and selective mGlu5 receptor antagonist with good rat pharmacokinetics, brain penetration, and in vivo receptor occupancy.
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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 antagonist
Bioorganic & Medicinal Chemistry Letters, 2004Co-Authors: Steve F Poon, Brian W Eastman, Deborah F Chapman, Janice Chung, Merryl Cramer, Gregory Holtz, Nicholas D P Cosford, Nicholas D SmithAbstract: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.
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2 2 3 pyridin 3 yloxy phenyl 2h tetrazol 5 yl pyridine a highly potent orally active metabotropic glutamate subtype 5 mglu5 receptor antagonist
Bioorganic & Medicinal Chemistry Letters, 2004Co-Authors: Dehua Huang, Steve F Poon, Deborah F Chapman, Janice Chung, Merryl Cramer, Nicholas D P Cosford, Thomas S Reger, Jeffrey Roger Roppe, Lida Tehrani, Nicholas D SmithAbstract:Abstract 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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discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity
Journal of Medicinal Chemistry, 2004Co-Authors: Jeffrey Roger Roppe, Janice Chung, Nicholas D Smith, Dehua Huang, Lida Tehrani, Bowei Wang, Jeffrey Anderson, Jesse Brodkin, Xiaohui Jiang, Christopher KingAbstract:The highly potent, selective, and brain-penetrant metabotropic glutamate subtype 5 (mGlu5) receptor antagonists 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile (47) and 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile (48) are reported. Compound 47 is active in the rat fear-potentiated startle (FPS) model of anxiety with ED50 = 5.4 mg/kg (po) when dosed acutely. In this model the anxiolytic effects of 47 rapidly tolerate on repeated dosing.
Janice Chung - One of the best experts on this subject based on the ideXlab platform.
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3 substituted 5 5 pyridin 2 yl 2h tetrazol 2 yl benzonitriles identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Lida R Tehrani, Steve F Poon, Deborah F Chapman, Janice Chung, Merryl Cramer, Nicholas D Smith, Dehua Huang, Jeffrey Roger Roppe, Thomas Jon Seiders, Nicholas D P CosfordAbstract:Structure-activity relationship studies on the phenyl ring of 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile 2 led to the discovery that small, non-hydrogen bond donor substituents at the 3-position led to a substantial increase in in vitro potency. In particular, 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile (7) is a highly potent and selective mGlu5 receptor antagonist with good rat pharmacokinetics, brain penetration, and in vivo receptor occupancy.
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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 antagonist
Bioorganic & Medicinal Chemistry Letters, 2004Co-Authors: Steve F Poon, Brian W Eastman, Deborah F Chapman, Janice Chung, Merryl Cramer, Gregory Holtz, Nicholas D P Cosford, Nicholas D SmithAbstract: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.
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2 2 3 pyridin 3 yloxy phenyl 2h tetrazol 5 yl pyridine a highly potent orally active metabotropic glutamate subtype 5 mglu5 receptor antagonist
Bioorganic & Medicinal Chemistry Letters, 2004Co-Authors: Dehua Huang, Steve F Poon, Deborah F Chapman, Janice Chung, Merryl Cramer, Nicholas D P Cosford, Thomas S Reger, Jeffrey Roger Roppe, Lida Tehrani, Nicholas D SmithAbstract:Abstract 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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discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity
Journal of Medicinal Chemistry, 2004Co-Authors: Jeffrey Roger Roppe, Janice Chung, Nicholas D Smith, Dehua Huang, Lida Tehrani, Bowei Wang, Jeffrey Anderson, Jesse Brodkin, Xiaohui Jiang, Christopher KingAbstract:The highly potent, selective, and brain-penetrant metabotropic glutamate subtype 5 (mGlu5) receptor antagonists 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile (47) and 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile (48) are reported. Compound 47 is active in the rat fear-potentiated startle (FPS) model of anxiety with ED50 = 5.4 mg/kg (po) when dosed acutely. In this model the anxiolytic effects of 47 rapidly tolerate on repeated dosing.
Jeffrey Roger Roppe - One of the best experts on this subject based on the ideXlab platform.
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3 substituted 5 5 pyridin 2 yl 2h tetrazol 2 yl benzonitriles identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Lida R Tehrani, Steve F Poon, Deborah F Chapman, Janice Chung, Merryl Cramer, Nicholas D Smith, Dehua Huang, Jeffrey Roger Roppe, Thomas Jon Seiders, Nicholas D P CosfordAbstract:Structure-activity relationship studies on the phenyl ring of 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile 2 led to the discovery that small, non-hydrogen bond donor substituents at the 3-position led to a substantial increase in in vitro potency. In particular, 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile (7) is a highly potent and selective mGlu5 receptor antagonist with good rat pharmacokinetics, brain penetration, and in vivo receptor occupancy.
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2 2 3 pyridin 3 yloxy phenyl 2h tetrazol 5 yl pyridine a highly potent orally active metabotropic glutamate subtype 5 mglu5 receptor antagonist
Bioorganic & Medicinal Chemistry Letters, 2004Co-Authors: Dehua Huang, Steve F Poon, Deborah F Chapman, Janice Chung, Merryl Cramer, Nicholas D P Cosford, Thomas S Reger, Jeffrey Roger Roppe, Lida Tehrani, Nicholas D SmithAbstract:Abstract 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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discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity
Journal of Medicinal Chemistry, 2004Co-Authors: Jeffrey Roger Roppe, Janice Chung, Nicholas D Smith, Dehua Huang, Lida Tehrani, Bowei Wang, Jeffrey Anderson, Jesse Brodkin, Xiaohui Jiang, Christopher KingAbstract:The highly potent, selective, and brain-penetrant metabotropic glutamate subtype 5 (mGlu5) receptor antagonists 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile (47) and 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile (48) are reported. Compound 47 is active in the rat fear-potentiated startle (FPS) model of anxiety with ED50 = 5.4 mg/kg (po) when dosed acutely. In this model the anxiolytic effects of 47 rapidly tolerate on repeated dosing.
Dehua Huang - One of the best experts on this subject based on the ideXlab platform.
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3 substituted 5 5 pyridin 2 yl 2h tetrazol 2 yl benzonitriles identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Lida R Tehrani, Steve F Poon, Deborah F Chapman, Janice Chung, Merryl Cramer, Nicholas D Smith, Dehua Huang, Jeffrey Roger Roppe, Thomas Jon Seiders, Nicholas D P CosfordAbstract:Structure-activity relationship studies on the phenyl ring of 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile 2 led to the discovery that small, non-hydrogen bond donor substituents at the 3-position led to a substantial increase in in vitro potency. In particular, 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile (7) is a highly potent and selective mGlu5 receptor antagonist with good rat pharmacokinetics, brain penetration, and in vivo receptor occupancy.
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2 2 3 pyridin 3 yloxy phenyl 2h tetrazol 5 yl pyridine a highly potent orally active metabotropic glutamate subtype 5 mglu5 receptor antagonist
Bioorganic & Medicinal Chemistry Letters, 2004Co-Authors: Dehua Huang, Steve F Poon, Deborah F Chapman, Janice Chung, Merryl Cramer, Nicholas D P Cosford, Thomas S Reger, Jeffrey Roger Roppe, Lida Tehrani, Nicholas D SmithAbstract:Abstract 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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discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity
Journal of Medicinal Chemistry, 2004Co-Authors: Jeffrey Roger Roppe, Janice Chung, Nicholas D Smith, Dehua Huang, Lida Tehrani, Bowei Wang, Jeffrey Anderson, Jesse Brodkin, Xiaohui Jiang, Christopher KingAbstract:The highly potent, selective, and brain-penetrant metabotropic glutamate subtype 5 (mGlu5) receptor antagonists 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile (47) and 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile (48) are reported. Compound 47 is active in the rat fear-potentiated startle (FPS) model of anxiety with ED50 = 5.4 mg/kg (po) when dosed acutely. In this model the anxiolytic effects of 47 rapidly tolerate on repeated dosing.
Nicholas D P Cosford - One of the best experts on this subject based on the ideXlab platform.
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3 substituted 5 5 pyridin 2 yl 2h tetrazol 2 yl benzonitriles identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Lida R Tehrani, Steve F Poon, Deborah F Chapman, Janice Chung, Merryl Cramer, Nicholas D Smith, Dehua Huang, Jeffrey Roger Roppe, Thomas Jon Seiders, Nicholas D P CosfordAbstract:Structure-activity relationship studies on the phenyl ring of 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile 2 led to the discovery that small, non-hydrogen bond donor substituents at the 3-position led to a substantial increase in in vitro potency. In particular, 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile (7) is a highly potent and selective mGlu5 receptor antagonist with good rat pharmacokinetics, brain penetration, and in vivo receptor occupancy.
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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 antagonist
Bioorganic & Medicinal Chemistry Letters, 2004Co-Authors: Steve F Poon, Brian W Eastman, Deborah F Chapman, Janice Chung, Merryl Cramer, Gregory Holtz, Nicholas D P Cosford, Nicholas D SmithAbstract: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.
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2 2 3 pyridin 3 yloxy phenyl 2h tetrazol 5 yl pyridine a highly potent orally active metabotropic glutamate subtype 5 mglu5 receptor antagonist
Bioorganic & Medicinal Chemistry Letters, 2004Co-Authors: Dehua Huang, Steve F Poon, Deborah F Chapman, Janice Chung, Merryl Cramer, Nicholas D P Cosford, Thomas S Reger, Jeffrey Roger Roppe, Lida Tehrani, Nicholas D SmithAbstract:Abstract 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.