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심영선,이예용,왕현정,태진성,박종현,추현아,임혜원,남길수 대한화학회 2023 Bulletin of the Korean Chemical Society Vol.44 No.7
A novel series of 4-arylthio- or 4-arylsulfonyl-substituted 2-amino-5,6,7,8- tetrahydroquiazolines was synthesized and evaluated for serotonin receptor subtype 6 (5-HT6R) antagonistic effects in vitro. The structure activity relationships (SAR) of this series were discussed on the basis of in vitro activity. Among the derivatives synthesized in the present study, the lead compound, 7a, having sulfonyl functionality at the 4-position and N-methylpiperazine at the 2-position of the core structure showed the most potent 5-HT6 receptor inhibitory activity in vitro and good metabolic stability without CYP liability.