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Synthesis and biological evaluation of all eight stereoisomers of DPP-IV inhibitor saxagliptin.

Abstract：

:All eight stereoisomers of saxagliptin have been synthesized and evaluated for their inhibitory activity against DPP-IV. It was unambiguously confirmed that the configuration of saxagliptin was critical to potent inhibition of DPP-IV. Docking study was performed to elucidate the configuration-activity relationship of saxagliptin stereoisomers. Tyr662 and Tyr470 have been suggested as the key residues of DPP-IV interacting with the inhibitors. This work provides valuable information for further inhibitor design against DPP-IV.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Dong J,Gong Y,Liu J,Chen X,Wen X,Sun H

doi

10.1016/j.bmc.2013.12.061

subject

Has Abstract

pub_date

2014-02-15 00:00:00

pages

1383-93

issue

4

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(13)01069-9

journal_volume

22

pub_type

杂志文章

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