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학술발표회초록보기

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제117회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Synthesis and biological activities of azetidine derivatives for discovery of S1P1R agonists

등록일
2016년 2월 24일 19시 09분 05초
접수번호
1882
발표코드
MEDI.P-475 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
4월 22일 (금요일) 13:00~14:30
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
이정은, 서선희1,*, 추현아2,*
고려대학교 화학과, Korea
1한국과학기술연구원(KIST) 뇌의약연구단, Korea
2한국과학기술연구원(KIST) 생명보건본부, Korea
Multiple sclerosis (MS) is an autoimmune disorder affecting the central nervous system. Immune cell attack the myelin sheaths of the central nervous system, leading to neurological distrurbance. Symptoms of multiple sclerosis may be single or multiple and may range from mild to severe in intensity and short to long in duration. Sphingosine 1-phosphate (S1P) signaling regulates immune cell egress from lymphoid organs into systemic circulation and prevents multiple sclerosis (MS) relapses. S1P1R agonists lead to a significant reduction of pheripheral blood lymphocyte (PBL) by internalization of S1P1R. Fingolimod (FTY720), an S1P1R agonist, was approved as the first oral drug for relapsing−remitting multiple sclerosis. FTY720 also agonizes other spingosine-1-phosphate (S1P) receptors (S1P3R, S1P4R, and S1P5R), It could cause diverse side effects such as bradycardia and electrical conductivity abnormalities which are linked exclusively to the S1P3R agonism. So our research is focused on developing S1P1R agonists with increased selectivity over the S1P3R to improve the safety profile. We designed, synthesized and biologically evaluated azetidine derivatives with benzene sulfonamide moiety. The results will be presented in detail.

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