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김주현,조용서,민선준 대한화학회 2016 Bulletin of the Korean Chemical Society Vol.37 No.12
A transition-metal-free and regioselective synthesis of a series of 2-amino-4-alkoxypyrimidines is described. The SNAr alkoxylation of 2,4-dichloropyrimidines regioselectively provided 2-chloro-4-alkoxypyrimidines, which were subsequently subject to the second SNAr amination with cyclic amines in the presence of triethylamine at high temperature to afford 2-amino-4-alkoxypyrimidines in good overall yield.
Synthesis and Biological Evaluation of N3-Alkyl-Thienopyrimidin-4-Ones as mGluR1 Antagonists
김민주,김영재,서선희,백두종,민선준,금교창,추현아 대한화학회 2015 Bulletin of the Korean Chemical Society Vol.36 No.5
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 N 3- 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 N 3-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.
Punna Reddy Ullapu,구수진,최연희,박지연,한소엽,백두종,이재균,배애님,민선준,조용서 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.8
The synthesis and biological evaluation of 1-heteroarylmethyl 1,4-diazepane derivatives as potential T-type calcium channel blockers is described. In this study, we have identified the compound 21i exhibiting the most potent T-type calcium channel blocking activity with IC_50 value of 0.20 μM, which is superior to that of mibefradil.
Synthesis of N-Alkyl-Carbazole Derivatives as 5-HT7R Antagonists
김영재,염미영,이소연,태진성,김학중,임혜원,성지혜,최경일,민선준,추현아 대한화학회 2018 Bulletin of the Korean Chemical Society Vol.39 No.9
We designed and synthesized a series of N-alkyl-carbazoles with different alkyl chains and amine moieties, and biological evaluation was performed to discover novel 5-HT7R antagonists. Among 27 synthesized compounds, 20, 21, 23, and 24 showed excellent binding affinities to 5-HT7R (Ki = 65, 64, 55, and 31 nM, respectively), and good selectivity profiles over other serotonin receptors. In functional assays, those compounds showed weak antagonistic activities against 5-HT7R. In particular, the compound 24, 2-(4-(5-(9H-carbazol-9-yl)pentyl)piperazin-1-yl)phenol, could be considered as a potent and selective 5-HT7R ligand with weak antagonistic effect. From the molecular docking study, the aromatic hydroxyl group in 24 was shown to play an important role in binding to 5-HT7R through a hydrogen bonding interaction with Asp142 in the ligand binding pocket of 5-HT7R.
Ji Young Kim,Myung-Hee Son,최기항,백두종,Min Kyung Ko,Eun Jeong Lim,배애님,금교창,Jae Kyun Lee,조용서,추현아,Youn-Woo Lee,문병석,이병철,이호영,민선준 대한화학회 2014 Bulletin of the Korean Chemical Society Vol.35 No.8
The synthesis and in vivo evaluation of 5-methoxy-2-(phenylethynyl)quinoline (MPEQ) 3 as a potential mGluR5 selective radioligand is described. We have identified MPEQ 3 exhibiting the analgesic effect in the neuropathic pain animal model. The effect of mGluR5 on neuronal activity in rat brain was evaluated through FDG/PET imaging in the presence of MPEQ 3. In addition, the PET study of [11C]MPEQ 3 proved that accumulation of [11C]MPEQ 3 in rat brain was correlated to the localization of the mGluR5.