期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 16, 期 22, 页码 9817-9829出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.09.060
关键词
mGluRs; Antagonist; Oral antagonistic activity
We describe here the discovery and the structure-activity relationship (SAR) of a series of 4-(1-Aryl-triazol-4- yl)-tetrahydropyridines as novel mGluR1 antagonists. Our extensive chemical modi. cation of lead compound 2 successfully led to fluoropyridine analogs 7j and 1 with improved in vivo antagonistic activities. Among the evaluated compounds, chemically stable urea analog 1 showed oral antagonistic activity at dose ranges of 10-30 mg/kg in an animal model. (C) 2008 Elsevier Ltd. All rights reserved.
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