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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Exhibition Hall 2+3 |
| Time |
10월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-307 |
| Subject |
Synthesis of azetidine-3-carboxylic acid derivatives as novel S1P1 agonists |
| Authors |
Jieon Lee, Hyunah Choo*, SEON HEE SEO
Center for Neuromedicine, Korea Institute of Science and Technology, Korea
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| Abstract |
Multiple sclerosis (MS) is an autoimmune disorder affecting central nervous system (CNS) in which the insulating covers of nerve cells in the brain and spinal cord are damaged, resulting in disrupting the ability of parts of the nervous system to communicate. Sphingosine-1-phosphate (S1P) is a bioactive sphingolipid that regulates a diverse range of physiological processes such as lymphocyte trafficking, cardiac function, vascular development, and inflammation. S1P receptors (S1PRs) are a class of G protein-coupled receptors, which are divided into five subtypes: S1P1, S1P2, S1P3, S1P4, and S1P5. Fingolimod (FTY720) as a S1P1 agonist was approved as the first oral drug for reducing relapse rate in multiple sclerosis. However, it also activates S1P3, S1P4 and S1P5 and causes various side effects such as bradycardia. Thus, we have focused on discovery of selective and potent S1P1 agonists. We designed and synthesized the compounds including azetidine-3-carboxylic acid and various biphenyl moiety. Synthesized compounds were biologically evaluated against S1P1. The results of in vitro assay and structure-activity relationship (SAR) will be presented in detail. |
| E-mail |
h16508@kist.re.kr |
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120th General Meeting of the KCS