Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3, 5-disubstituted-phenyl series

…, H DaCosta, Y Chen, K Hemstapat, A Rodriguez…

文献索引：Alagille, David; Dacosta, Herve; Chen, Yelin; Hemstapat, Kamondanai; Rodriguez, Alice; Baldwin, Ronald M.; Conn, Jeffrey P.; Tamagnan, Gilles D. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3243 - 3247

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被引用次数: 12

摘要

Abstract We report the synthesis of four series of 3, 5-disubstituted-phenyl ligands targeting the metabotropic glutamate receptor subtype 5:(2-methylthiazol-4-yl) ethynyl (1a–j,),(6- methylpyridin-2-yl) ethynyl (2a–j),(5-methylpyridin-2-yl) ethynyl (3a–j,), and (pyridin-2-yl) ethynyl (4a–j,). The compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. All compounds were found to ...