Synthesis and Biological Evaluation of N3-Alkyl-Thienopyrimidin-4-Ones as mGluR1 Antagonists
- Synthesis and Biological Evaluation of N3-Alkyl-Thienopyrimidin-4-Ones as mGluR1 Antagonists
- 김민주; 김영재; 서선희; 백두종; 민선준; 금교창; 추현아
- mGluR1 antagonist; N3-Alkyl-thienopyrimidin-4-one; CNS disease; Neuropathic pain; Glutamate
- Issue Date
- Bulletin of the Korean Chemical Society
- VOL 36, NO 5, 1439-1451
- Metabotropic glutamate receptor subtype 1 (mGluR1) is a potential target for the treatment of neuropathic pain, and there has been much effort to discover mGluR1 antagonists. In this study, a series of N3-alkyl-thienopyrimidin-4-ones were prepared by introducing various alkyl and aryl groups to the N3- and 7-positions of the thienopyrimidin-4-one core structure, respectively, and their inhibitory activities against mGluR1 were biologically evaluated. Structure–activity relationship study revealed that the trans-4-methylcyclohexyl, cycloheptyl, and cyclooctyl groups at N3-position, and 2-fluorophenyl group at 7-position were most effective in potentiating the inhibitory activity of the thienopyrimidin-4-one derivatives against mGluR1. Among the synthesized compounds, 3-cyclooctyl-7-phenylthienopyrimidin-4-one and 3-cycloheptyl-7-(2-fluorophenyl) thienopyrimidin-4-one exhibited the most potent inhibitory activities with IC50 values of 115 and 107 nM, respectively.
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