1. Academic Validation
  2. Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors

Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors

  • Bioorg Med Chem Lett. 2011 Jun 15;21(12):3774-9. doi: 10.1016/j.bmcl.2011.04.053.
Xiaohui Du 1 Mike Lizarzaburu Simon Turcotte Taeweon Lee Joanne Greenberg Bei Shan Peter Fan Yun Ling Julio C Medina Jonathan Houze
Affiliations

Affiliation

  • 1 Amgen Inc., South San Francisco, CA 94080, USA. xdu@amgen.com
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.

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