120th General Meeting of the KCS

Type Poster Presentation
Area Medicinal Chemistry
Room No. Exhibition Hall 2+3
Time 10월 19일 (목요일) 11:00~12:30
Code MEDI.P-318
Subject Synthesis of biphenyl-3-ylmethylamine derivatives as 5-HT7 receptor modulators
Authors Soyeon Lee, Youngjae Kim1, Hak Joong Kim, Hyunah Choo2,*
Department of Chemistry, Korea University, Korea
1Department of Chemistry, Yonsei University, Korea
2Korea Institute of Science and Technology, Korea
Abstract 5-HT7 receptor is the most recently discovered serotonin receptor that localized within CNS such as thalamus, hypothalamus, limbic and cortical regions. Recent reports suggest that 5-HT7 receptor is involved in the regulation of body temperature, circadian rhythms, learning and memory, as well as neuronal excitability, inflammatory processes and smooth muscle relaxation of cerebral arteries. 5-HT7 receptor knockout animal studies have provided demonstrative proofs that 5-HT7 receptor is considered as a potential target for treating depression, sleep disorder, and neuropathic pain. There has been much attention to discover 5-HT7 modulators to obtain therapeutic benefits. We have designed and synthesized compounds including biphenyl-3-ylmethylamines. Using Suzuki reaction and reductive amination, total 12 final compounds with biphenyl moiety were synthesized and biologically evaluated against 5-HT7 receptor. Among them, two compounds showed the best binding affinities with Ki values of 9.3 and 6.8 nM, respectively. The results of binding affinity assay and structure-activity relationship (SAR) to 5-HT7 receptors will be presented in detail.
E-mail 117018@kist.re.kr