Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists

…, R Wouters, ASJ Lesage, LV Beijsterveldt…

文献索引：Mabire, Dominique; Coupa, Sophie; Adelinet, Christophe; Poncelet, Alain; Simonnet, Yvan; Venet, Marc; Wouters, Ria; Lesage, Anne S. J.; Van Beijsterveldt, Ludy; Bischoff, Francois Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 2134 - 2153

全文：HTML全文

被引用次数: 68

摘要

We describe the discovery and the structure-activity relationship of a new series of quinoline derivatives acting as selective and highly potent noncompetitive mGlu1 antagonists. We first identified cis-10 as a fairly potent mGlu1 antagonist (IC50= 20 nM) in a cell-based signal transduction assay on the rat mGlu1 receptor expressed in CHO-K1 cells, and then we were able to design and synthesize highly potent compounds on both rat and human mGlu1 ...