Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones

We have identified and synthesized a series of aryl-tetrazoyl acetophenones as positive allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation led to the discovery of 22 (EC(50)=93nM, 1...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-11, Vol.14 (21), p.5329-5332
Main Authors: PINKERTON, Anthony B, CUBE, Rowena V, HUTCHINSON, John H, ROWE, Blake A, SCHAFFHAUSER, Hervé, XIUMIN ZHAO, DAGGETT, Lorrie P, VERNIER, Jean-Michel
Format: Article
Language:English
Subjects:
Acetophenones - chemical synthesis
Acetophenones - chemistry
Acetophenones - pharmacology
Allosteric Regulation
Biological and medical sciences
Glutamatergic system (aspartate and other excitatory aminoacids)
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Receptors, Metabotropic Glutamate - agonists
Stereoisomerism
Structure-Activity Relationship
Tetrazoles - chemical synthesis
Tetrazoles - chemistry
Tetrazoles - pharmacology
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Summary:We have identified and synthesized a series of aryl-tetrazoyl acetophenones as positive allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation led to the discovery of 22 (EC(50)=93nM, 128% potentiation).
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.08.020