Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 22, Issue 4, Pages 1383-1393Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.12.061
Keywords
Saxagliptin; Stereoisomers; Synthesis; Configuration-activity relationship; DPP-IV inhibitors
Funding
- Ministry of Education of China
- State Administration of Foreign Expert Affairs of China [111-2-07]
- Program for Changjiang Scholars and Innovative Research Team in University [IRT1193]
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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. (C) 2014 Elsevier Ltd. All rights reserved.
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