Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors

  • Du X
  • Lizarzaburu M
  • Turcotte S
 et al. 
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Abstract

Previous efforts have led to the identification of a potent, selective, and nonphlorizin based SGLT2 inhibitor 1. This Letter describes efforts to further optimize the potency, microsomal stability, solubility and pharmacokinetic properties of this series of SGLT2 inhibitors. From these efforts, compounds 28 and 32 have improved solubility and pharmacokinetic properties compared to compound 1. © 2011 Elsevier Ltd. All rights reserved.

Author-supplied keywords

  • Benzooxazinone head groups
  • Indane tail group
  • Noncompetitive SGLT2 inhibitors
  • SAR
  • Solubility
  • Triazoles

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Authors

  • Xiaohui Du

  • Mike Lizarzaburu

  • Simon Turcotte

  • Taeweon Lee

  • Joanne Greenberg

  • Bei Shan

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