… of ((4 R, 5 S)-5-Amino-4-(2, 4, 5-trifluorophenyl) cyclohex-1-enyl)-(3-(trifluoromethyl)-5, 6-dihydro-[1, 2, 4] triazolo [4, 3-a] pyrazin-7 (8 H)-yl) methanone (ABT-341), a …

…, K Longenecker, H Yong, TH Lubben…

文献索引：Pei, Zhonghua; Li, Xiaofeng; Von Geldern, Thomas W.; Madar, David J.; Longenecker, Kenton; Yong, Hong; Lubben, Thomas H.; Stewart, Kent D.; Zinker, Bradley A.; Backes, Bradley J.; Judd, Andrew S.; Mulhern, Mathew; Ballaron, Stephen J.; Stashko, Michael A.; Mika, Amanda K.; Beno, David W. A.; Reinhart, Glenn A.; Fryer, Ryan M.; Preusser, Lee C.; Kempf-Grote, Anita J.; Sham, Hing L.; Trevillyan, James M. Journal of Medicinal Chemistry, 2006 , vol. 49, # 22 p. 6439 - 6442

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被引用次数: 48

摘要

Dipeptidyl peptidase IV (DPP4) deactivates glucose-regulating hormones such as GLP-1 and GIP, thus, DPP4 inhibition has become a useful therapy for type 2 diabetes. Optimization of the high-throughput screening lead 6 led to the discovery of 25 (ABT-341), a highly potent, selective, and orally bioavailable DPP4 inhibitor. When dosed orally, 25 dose- dependently reduced glucose excursion in ZDF rats. Amide 25 is safe in a battery of in ...