2. Academic Validation
  3. The design and synthesis of novel SGLT2 inhibitors: C-glycosides with benzyltriazolopyridinone and phenylhydantoin as the aglycone moieties

The design and synthesis of novel SGLT2 inhibitors: C-glycosides with benzyltriazolopyridinone and phenylhydantoin as the aglycone moieties

  • Bioorg Med Chem. 2014 Jul 1;22(13):3414-22. doi: 10.1016/j.bmc.2014.04.036.
Cheng Guo 1,  Min Hu 1,  Russell J DeOrazio 1,  Alexander Usyatinsky 1,  Kevin Fitzpatrick 1,  Zhenjun Zhang 1,  Jun-Ho Maeng 1,  Douglas B Kitchen 1,  Susan Tom 1,  Michele Luche 1,  Yuri Khmelnitsky 1,  Andrew J Mhyre 1,  Peter R Guzzo 1,  Shuang Liu 2
Affiliations

Affiliations

  • 1 AMRI, 26 Corporate Circle, PO Box 15098, Albany, NY 12212-5098, USA.
  • 2 AMRI, 26 Corporate Circle, PO Box 15098, Albany, NY 12212-5098, USA. Electronic address: shuang.Liu@amriglobal.com.
PMID: 24842618 DOI: 10.1016/j.bmc.2014.04.036
Abstract

The sodium glucose co-transporter 2 (SGLT2) has received considerable attention in recent years as a target for the treatment of type 2 diabetes mellitus. This report describes the design, synthesis and structure-activity relationship (SAR) of C-glycosides with benzyltriazolopyridinone and phenylhydantoin as the aglycone moieties as novel SGLT2 inhibitors. Compounds 5p and 33b demonstrated high potency in inhibiting SGLT2 and high selectivity against SGLT1. The in vitro ADMET properties of these compounds will also be discussed.

Keywords

Canagliflozin; Dapagliflozin; Glucoside; Hydantoin; SGLT2; Triazolopyridinone.

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