Design, synthesis and biological evaluation of novel pyrazolo-pyrimidinones as DPP-IV inhibitors in diabetes.
作者： Sneha R. Sagar , Jessica K. Agarwal , Dhaivat H. Pandya , Ranjeet Prasad Dash , Manish Nivsarkar
DOI: 10.1016/J.BMCL.2015.09.015
关键词: Enzyme 、 Structure–activity relationship 、 In vitro 、 Biological activity 、 Dipeptidyl peptidase-4 、 Docking (molecular) 、 In vivo 、 Chemistry 、 Biochemistry 、 Pyrimidinones
摘要: We report the design, synthesis, biological activity and docking studies of series novel pyrazolo[3,4-d]pyrimidinones as DPP-IV inhibitors in diabetes. Molecules were synthesized evaluated for their inhibition activity. Compounds 5e, 5k, 5o 6a found to be potent enzyme. Amongst all compounds, 6-methyl-5-(4-methylpyridin-2-yl)-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one (5k) was most active based on vitro also exhibited promising vivo blood glucose lowering male Wistar rats.
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