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  • 08월 28일 16시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

Design and Synthesis of Quinoline Derivatives as a Novel Class of Acyl CoA: Cholestrol Acyl Transferase (ACAT) Inhibitors

등록일
2008년 8월 11일 18시 18분 33초
접수번호
0762
발표코드
35P301포 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
목 <발표Ⅰ>
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
구자일, 이성윤1, 이승웅2, 노문철3, 김영국4, 최용석5
고려대학교 의약생명공학과, Korea
1생명과학대학, Korea
2한국생명공학연구원 천연물의약연구센타, Korea
3한국생명공학연구원 바이오의약연구부, Korea
4한국생명공학연구원 천연물연구센터, Korea
5고려대학교 생명과학대학, Korea
A series of novel quinoline derivatives were synthesized as potential ACAT inhibitors. Acyl-coenzyme A:cholesterol acyltransferase (ACAT) is an intracellular enzyme that catalyzes the conjugation of long chain fatty acid and cholesterol to form cholesteryl esters and related to the production of lipoproteins and accumulation of chlolestreyl esters of the atheroma. Therefore, ACAT inhibitors have long been sought as potential therapeutics for hypercholesterinemia and atherosclerosis. Recently, it was reported that shikonin derivatives with naphthoquinone template possessed ACAT inhibitory activity in vitro as well as cell-based assay system. Based on the activity of the naphthoquinone template, it was of interest to synthesize quinoline-based derivatives as potential ACAT inhibitors and it was found that N-substituted quinolin carboxamide derivatives showed interesting ACAT inhibitory activity. Structure-activity relationships of quinoline analogues as ACAT inhibitors will be presented.

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