Palladium-Catalyzed Arylation of Carbasugars Enables the Discovery of Potent and Selective SGLT2 Inhibitors

Wai Lung Ng, Kit Man Lau, Clara B.S. Lau, Tony Kung Ming Shing

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

Selective inhibition of the transporter protein sodium-glucose cotransporter 2 (SGLT2) has emerged as a promising way to control blood glucose level in diabetes patients. Reported herein is a short and convergent synthetic route towards some small-molecule SGLT2 inhibitors by a chemo- and diastereospecific palladium-catalyzed arylation reaction. This synthetic strategy enabled the discovery of two highly selective and potent SGLT2 inhibitors, thereby paving the way towards the development of carbasugar SGLT2 inhibitors as potential antidiabetic/antitumor agents.

Original languageEnglish
Pages (from-to)13818-13821
Number of pages4
JournalAngewandte Chemie - International Edition
Volume55
Issue number44
DOIs
Publication statusPublished - 2016 Jan 1
Externally publishedYes

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Keywords

  • carbohydrates
  • cross-coupling
  • drug design
  • inhibitors
  • palladium

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)

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