Discovery of ((4R,5S)-5-Amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a Highly Potent, Selective, Orally Efficacious, and Safe Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

作者： Zhonghua Pei , Xiaofeng Li , Thomas W. von Geldern , David J. Madar , Kenton Longenecker

关键词: Structure–activity relationship 、 Chemistry 、 Dipeptidyl peptidase 、 Trifluoromethyl 、 Oral administration 、 Carboxamide 、 Enzyme inhibitor 、 Pharmacology 、 Stereochemistry 、 In vivo 、 Pharmacokinetics 、 Molecular medicine 、 Drug discovery

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 discovery 25 (ABT-341), highly potent, selective, orally bioavailable inhibitor. When dosed orally, dose-dependently reduced glucose excursion in ZDF rats. Amide is safe battery vitro vivo tests may represent new therapeutic agent treatment

参考文章(0)

Discovery of ((4R,5S)-5-Amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a Highly Potent, Selective, Orally Efficacious, and Safe Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

来源期刊

我的账户

Discovery of ((4R,5S)-5-Amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a Highly Potent, Selective, Orally Efficacious, and Safe Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

来源期刊

相似文章 10

我的账户