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Discovery of canagliflozin, a novel C-glucoside with thiophene ring, as sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes mellitus. | LitMetric

AI Article Synopsis

  • Researchers found that C-glucosides with a heteroaromatic ring are more stable as SGLT2 inhibitors compared to O-glucosides.
  • The study identified a new compound, a thiophene derivative known as canagliflozin, which is an effective SGLT2 inhibitor.
  • Canagliflozin exhibited strong anti-hyperglycemic effects in mice fed a high-fat diet.

Article Abstract

We discovered that C-glucosides 4 bearing a heteroaromatic ring formed metabolically more stable inhibitors for sodium-dependent glucose cotransporter 2 (SGLT2) than the O-glucoside, 2 (T-1095). A novel thiophene derivative 4b-3 (canagliflozin) was a highly potent and selective SGLT2 inhibitor and showed pronounced anti-hyperglycemic effects in high-fat diet fed KK (HF-KK) mice.

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Source
http://dx.doi.org/10.1021/jm100332nDOI Listing

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