(3-substituted benzyl)thiazolidine-2,4-diones as structurally new antihyperglycemic agents.
作者： Masahiro Nomura , Susumu Kinoshita , Hiroya Satoh , Toshio Maeda , Koji Murakami
DOI: 10.1016/S0960-894X(99)00039-6
关键词: Chemistry 、 Trifluoromethyl 、 Antihyperglycemic Agents 、 Non insulin dependent diabetes mellitus 、 Antidiabetic agents 、 Thiazolidine 、 Carboxamide 、 Stereochemistry 、 Chemical synthesis 、 Benzamide
摘要: A series of 3-[(2,4-dioxothiazolidin-5-yl)methyl]benzamide derivatives was prepared as part a search for antidiabetic agents. structure-activity relationship study these compounds led to the identification 5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[[4-(trifluoromethyl)-phenyl]methyl]benzamide (KRP-297) candidate drug treatment diabetes mellitus.
elsevier.com
sci-hub.se 参考文章(13)
Takao Yoshioka, Takashi Fujita, Tsutomu Kanai, Yuichi Aizawa, Tomoyuki Kurumada, Kazuo Hasegawa, Hiroyoshi Horikoshi, STUDIES ON HINDERED PHENOLS AND ANALOGUE. HYPOLIPIDEMIC AND HYPOGLYCAEMIC AGENTS WITH ABILITY TO INHIBIT LIPID PEROXIDATION Journal of Medicinal Chemistry. ,vol. 32, pp. 421- 427 ,(1989) , 10.1021/JM00122A022
Jürgen M. Lehmann, Linda B. Moore, Tracey A. Smith-Oliver, William O. Wilkison, Timothy M. Willson, Steven A. Kliewer, An Antidiabetic Thiazolidinedione Is a High Affinity Ligand for Peroxisome Proliferator-activated Receptor γ (PPARγ) Journal of Biological Chemistry. ,vol. 270, pp. 12953- 12956 ,(1995) , 10.1074/JBC.270.22.12953
Jonathan B. Jaspan, Monitoring and controlling the patient with non-insulin-dependent diabetes mellitus Metabolism-clinical and Experimental. ,vol. 36, pp. 22- 27 ,(1987) , 10.1016/0026-0495(87)90197-1
K Dahl-Jorgensen, O Brinchmann-Hansen, K F Hanssen, T Ganes, P Kierulf, E Smeland, L Sandvik, O Aagenaes, Effect of near normoglycaemia for two years on progression of early diabetic retinopathy, nephropathy, and neuropathy: the Oslo study. BMJ. ,vol. 293, pp. 1195- 1199 ,(1986) , 10.1136/BMJ.293.6556.1195
Yu MOMOSE, Kanji MEGURO, Hitoshi IKEDA, Chitoshi HATANAKA, Satoru OI, Takashi SOHDA, Studies on antidiabetic agents. X. Synthesis and biological activities of pioglitazone and related compounds Chemical & Pharmaceutical Bulletin. ,vol. 39, pp. 1440- 1445 ,(1991) , 10.1248/CPB.39.1440
R. W. Stevenson, N. J. Hutson, M. N. Krupp, R. A. Volkmann, G. F. Holland, J. F. Eggler, D. A. Clark, R. K. McPherson, K. L. Hall, B. H. Danbury, E. M. Gibbs, D. K. Kreutter, Actions of novel antidiabetic agent englitazone in hyperglycemic hyperinsulinemic ob/ob mice. Diabetes. ,vol. 39, pp. 1218- 1227 ,(1990) , 10.2337/DIAB.39.10.1218
K. Murakami, K. Tobe, T. Ide, T. Mochizuki, M. Ohashi, Y. Akanuma, Y. Yazaki, T. Kadowaki, A novel insulin sensitizer acts as a coligand for peroxisome proliferator-activated receptor-alpha (PPAR-alpha) and PPAR-gamma: effect of PPAR-alpha activation on abnormal lipid metabolism in liver of Zucker fatty rats. Diabetes. ,vol. 47, pp. 1841- 1847 ,(1998) , 10.2337/DIABETES.47.12.1841
TAKASHI SOHDA, KATSUTOSHI MIZUNO, HIROYUKI TAWADA, YASUO SUGIYAMA, TAKESHI FUJITA, YUTAKA KAWAMATSU, Studies on antidiabetic agents. I. Synthesis of 5-[4-(2-methyl-2-phenylpropoxy)-benzyl]thiazolidine-2,4-dione (AL-321) and related compounds. Chemical & Pharmaceutical Bulletin. ,vol. 30, pp. 3563- 3573 ,(1982) , 10.1248/CPB.30.3563
The effect of intensive treatment of diabetes on the development and progression of long-term complications in insulin-dependent diabetes mellitus. The New England Journal of Medicine. ,vol. 329, pp. 977- 986 ,(1993) , 10.1056/NEJM199309303291401
D. Porte Jr., M. W. Schwartz, Diabetes Complications--Why Is Glucose Potentially Toxic? Science. ,vol. 272, pp. 699- 700 ,(1996) , 10.1126/SCIENCE.272.5262.699