Shim, Young Sun Lee, Yeyong Wang, Hyun Jung Tae, Jinsung Park, Jonghyun Choo, Hyunah Rhim, Hyewhon Nam, Ghilsoo 2024-01-19T09:05:15Z 2024-01-19T09:05:15Z 2023-05-18 2023-07 0253-2964 https://pubs.kist.re.kr/handle/201004/113561 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. English 대한화학회 Synthesis and structure activity relationship studies of 2-amino-4-arylysulfonyl-5,6,7,8-tetrahydroquinazolines as 5-HT6 receptor antagonists Article 10.1002/bkcs.12696 1 Bulletin of the Korean Chemical Society, v.44, no.7, pp.572 - 577 Bulletin of the Korean Chemical Society 44 7 572 577 N scie scopus kci ART002981837 000976754900001 2-s2.0-85153527220 Chemistry, Multidisciplinary Chemistry Article 2-amino-4-arylysulfonyl-5,6,7,8-tetrahydroquiazolines 5-HT6 receptor antagonist CYP HLM stability SAR