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Design, synthesis and biological evaluation of novel pyrazolo-pyrimidinones as DPP-IV inhibitors in diabetes.

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. Compounds 5e, 5k, 5o and 6a were found to be potent inhibitors of DPP-IV enzyme. Amongst all the synthesized compounds, 6-methyl-5-(4-methylpyridin-2-yl)-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Sagar SR,Agarwal JK,Pandya DH,Dash RP,Nivsarkar M,Vasu KK

doi

10.1016/j.bmcl.2015.09.015

subject

Has Abstract

pub_date

2015-10-15 00:00:00

pages

4428-33

issue

20

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)30049-4

journal_volume

25

pub_type

杂志文章

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