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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Event Hall |
| Time |
4월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-598 |
| Subject |
Synthesis and biological evaluation of biaryl-3-ylmethylamine derivatives as 5-HT1A 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
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| Abstract |
5-HT1A receptor is the most widespread among all the 5-HT receptors, which is localized within blood vessel and CNS such as cerebral cortex, hippocampus, and raphe nucleus. Recent reports suggest that 5-HT1A receptor is involved in blood pressure, heart rate, anxiety, memory, etc. 5-HT1A receptor ligands can act as analgesics, antidepressants, anxiolytics, and nootropics. There has been much attention to discover 5-HT1A modulators to obtain therapeutic benefits. We have designed and synthesized compounds including biaryl-3-ylmethylamines. Using Suzuki reaction, reductive amination and amide coupling, total 28 final compounds with biaryl moiety were synthesized and biologically evaluated against 5-HT1A receptor. The results of binding affinity assay and structure-activity relationship (SAR) to 5-HT1Areceptors will be presented in detail. |
| E-mail |
117018@kist.re.kr |
|
121st General Meeting of the KCS