Structure−Activity Relationship of Triazafluorenone Derivatives as Potent and Selective mGluR1 Antagonists
Journal of Medicinal Chemistry2005Vol. 48(23), pp. 7374–7388
Citations Over TimeTop 18% of 2005 papers
Guo Zhu Zheng, Pramila Bhatia, Jerome F. Daanen, Teodozyj Kolasa, Meena Patel, Steven P. Latshaw, Odile F. El Kouhen, Renjie Chang, Marie E. Uchic, Loan Miller, Masaki Nakane, Sonya G. Lehto, Marie P. Honore, Robert B. Moreland, Jorge D. Brioni, Andrew O. Stewart
Abstract
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 antagonists. Compound 1n, for example, was a very potent mGluR1 antagonist (IC50 = 3 nM) and demonstrated full efficacy in various in vivo animal pain models.
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