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J Med Chem. 2005 Nov 17;48(23):7374-88.

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

Author information

1
Neuroscience Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064-6115, USA. Guozhu.zheng@Abbott.com

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.

PMID:
16279797
DOI:
10.1021/jm0504407
[Indexed for MEDLINE]

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