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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-326 |
| Subject |
Synthesis and Biological Activity of Tetrahydroisoxazolopyridine as S1P1 Receptor Agonist |
| Authors |
Young Jin Choi, Ji Soo Seo1, SEON HEE SEO 2, Ghilsoo Nam3,*
Division of Bio-Med, University of Science & Technology, Korea
1department of chemistry, Kyung Hee University, Korea
2Center for Neuromedicine, Korea Institute of Science and Technology, Korea
3Korea Institute of Science and Technology, Korea
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| Abstract |
Multiple Sclerosis(MS) is an inflammatory and chronic disease of the CNS. MS is a demyelinating disease in which the insulating covers of nerve cells in the brain and spinal cord are damaged. This damage disrupts the ability of parts of the nervous system to communicate. In 2010, Novatis developed the first oral drug Fingolimod as a S1P receptor agonist. Fingolimod binds S1P1receptor and effects as a functional antagonist. Initially, the ligand binds S1P receptor-1(S1P1R) and then leads to internalization of S1P1R on T-cells. Down-regulation of S1P1R on lymph node T-cells renders lymphocytes unresponsive to the egressive signal and therefore prevents infiltration of pathogenic T-cells into the CNS. However, Fingolimod is a non-selective S1P1R and then induces several side effects such as bradycardia(when Fingolimod binds S1P3R). In this study, we tried to design new structures for compounds selectively bind to S1P1R and S1P5R agonist on the basis of the structure of BAF-312. In this poster, synthesis and biological activity tetrahydroisoxazolopyridine compounds as S1P1 receptor agonist are described. |
| E-mail |
H14508@kist.re.kr |
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120th General Meeting of the KCS