Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists

GZ Zheng, P Bhatia, J Daanen, T Kolasa…

文献索引：Zheng, Guo Zhu; Bhatia, Pramila; Daanen, Jerome; Kolasa, Teodozyj; Patel, Meena; Latshaw, Steven; El Kouhen, Odile F.; Chang, Renjie; Uchic, Marie E.; Miller, Loan; Nakane, Masaki; Lehto, Sonya G.; Honore, Marie P.; Moreland, Robert B.; Brioni, Jorge D.; Stewart, Andrew O. Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7374 - 7388

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被引用次数: 61

摘要

SAR (structure-activity relationship) studies of triazafluorenone derivatives as potent mGluR1 antagonists are described. The triazafluorenone derivatives are non-amino acid derivatives and noncompetitive mGluR1 antagonists that bind at a putative allosteric recognition site located within the seven-transmembrane domain of the receptor. These triazafluorenone derivatives are potent, selective, and systemically active mGluR1 ...