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제118회 대한화학회 학술발표회, 총회 및 기기전시회 안내 SYNTHESIS AND BIOLOGICAL EVALUATION OF PYRIMIDINE DERIVATIVES AS GPR119 AGONISTS

등록일
2016년 8월 29일 16시 32분 30초
접수번호
2130
발표코드
MEDI.P-502 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
10월 13일 (목요일) 11:00~12:30
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
김효진, 유민진1, 정관영2,*
서강대학교 화학과, Korea
1과학기술연합대학원대학교(UST) 한국화학연구원/의약화학, Korea
2한국화학연구원 의약화학연구센터, Korea
Diabetes is a serious metabolic disorder that occurs when the pancreas does not produce enough insulin, or the body cannot effectively use existing insulin. Hyperglycemia (high blood glucose) can lead to various health consequences such as kidney damage, heart disease, stroke, nerve damage and blindness. Type 2 diabetes mellitus (T2DM, or noninsulin dependent), is the most common form of diabetes caused by insulin resistance, and loss of pancreatic ß-cell function and approximately 95% diabetic patients are suffering from type 2 diabetes. GPR119 is a member of the class A G protein-coupled receptor (GPCR) family, and it is highly expressed in pancreatic ß-cells and intestinal endocrine cells. Upon activation by its endogenous ligand, intracellular cAMP accumulates and adenylate cyclase activation enhances the effect of glucose-stimulated insulin secretion (GSIS) and GLP-1 release. Thus GPR119 represents a promising target for the treatment of type 2 diabetes and obesity owing to its ability to improve glucose homoeostasis while concurrently slowing gastric emptying, reducing food intake and promoting weight loss Endogenous ligands for GPR-119 have been identified including lysophosphatidylcholine (LPC) and oleoylethanolamide (OEA). When Sanofi-Aventis agreed to get the right of MBX-2982 from Metabolex (Cymabay Therapeutics) in 2010, which was a representative orally active GPR119 agonist. However, Sanofi-Aventis opted to terminate the deal in May 2011, has a loss of efficacy durig its clinical trial. We looked in deeply of MBX-2982 and substituted tetrazole moiety to five-membered heterocylic ring which increased the activity (five-fold potent) and metabolic stability. Also, we modified ethylpyrimidine side of MBX-2982 with polar linkers

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