3-[Substituted]-5-(5-pyridin-2-yl-2 H-tetrazol-2-yl)benzonitriles: Identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists

Structure–activity relationship studies on the phenyl ring of 3-(5-pyridin-2-yl-2 H-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-2 H-te...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-11, Vol.15 (22), p.5061-5064
Hauptverfasser:	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.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antagonist Biological and medical sciences Brain - drug effects Brain - metabolism Excitatory Amino Acid Antagonists - chemical synthesis Excitatory Amino Acid Antagonists - chemistry Excitatory Amino Acid Antagonists - pharmacology Glutamatergic system (aspartate and other excitatory aminoacids) Kinetics Medical sciences Metabotropic glutamate receptor 5 Mice Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Nitriles - chemistry Nitriles - pharmacology Occupancy Pharmacology. Drug treatments Pyridines - chemistry Rats Receptor, Metabotropic Glutamate 5 Receptors, Metabotropic Glutamate - antagonists & inhibitors Receptors, Metabotropic Glutamate - metabolism Sensitivity and Specificity Structure-Activity Relationship Substrate Specificity Tetrazole Tetrazoles - chemistry
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