Design, synthesis and biological evaluation of novel pyrazolo-pyrimidinones as DPP-IV inhibitors in diabetes. Issue 20 (15th October 2015)

• Record Type: Journal Article
• Authors: Sagar, Sneha R.; Agarwal, Jessica K.; Pandya, Dhaivat H.; Dash, Ranjeet Prasad; Nivsarkar, Manish; Vasu, Kamala K.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 20(2015)
• Page Start: 4428
• Page End: 4433
• Publication Date: 2015-10-15
• Subjects: DPP-IV enzyme -- Pyrazolo-pyrimidinones -- Molecular docking; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.09.015
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: We report the design, synthesis, biological activity and docking studies of series of novel pyrazolo[3, 4- d ]pyrimidinones as DPP-IV inhibitors in diabetes. Molecules were synthesized and evaluated for their DPP-IV inhibition activity. Compounds5e, 5k, 5o and6a were found to be potent inhibitors of DPP-IV enzyme. Amongst all the synthesized compounds, 6-methyl-5-(4-methylpyridin-2-yl)-1-phenyl-1 H -pyrazolo[3, 4- d ]pyrimidin-4(5 H )-one (5k ) was found to be the most active based on in vitro DPP-IV studies and also exhibited promising in vivo blood glucose lowering activity in male Wistar rats.