Synthesis and receptor assay of aromatic–ethynyl–aromatic derivatives with potent mGluR5 antagonist activity

D Alagille, RM Baldwin, BL Roth, JT Wroblewski…

文献索引：Alagille, David; Baldwin, Ronald M.; Roth, Bryan L.; Wroblewski, Jarda T.; Grajkowska, Ewa; Tamagnan, Gilles D. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 1 p. 197 - 209

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被引用次数: 40

摘要

Noncompetitive antagonists of the human metabotropic glutamate receptor subtype 5 (mGluR5) have been implicated as potential therapeutics for the treatment of a variety of nervous system disorders, including pain, anxiety, and drug addiction. To discover novel noncompetitive antagonists to the mGluR5, we initiated an SAR study around the known lead compounds MPEP and M-MPEP. Our results pointed out the critical role of the para ...