Synthetic strategy and SAR studies of C-glucoside heteroaryls as SGLT2 inhibitor: A review

Eur J Med Chem. 2019 Dec 15;184:111773. doi: 10.1016/j.ejmech.2019.111773. Epub 2019 Oct 12.


Gliflozins constitute an important class of compounds useful as sodium glucose co-transporter (SGLT2) inhibitors to treat type-II diabetes. They act by blocking sodium-glucose transport protein 2 which is responsible for re-absorption of glucose in the proximal convoluted tubule (PCT) of kidney and thus its inhibition reduces blood glucose level. There are a number of gliflozins which have been approved by drug regulatory bodies like FDA, EMA and PMDA whereas some others are in pipeline in their late developmental phases. The present review article offers a detailed account of synthetic strategies employed for the synthesis, alternate synthetic routes along with Structure Activity Relationship (SAR) studies of well-established as well as newly developed SGLT2 inhibitors.

Keywords: Diabetes mellitus; SGLT2 inhibitors; Structure activity relationship; Urinary glucose excretion.

Publication types

  • Review

MeSH terms

  • Animals
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetes Mellitus, Type 2 / metabolism
  • Dose-Response Relationship, Drug
  • Glucosides / chemical synthesis
  • Glucosides / chemistry
  • Glucosides / pharmacology*
  • Humans
  • Hypoglycemic Agents / chemical synthesis
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacology*
  • Molecular Structure
  • Sodium-Glucose Transporter 2 / metabolism*
  • Sodium-Glucose Transporter 2 Inhibitors / chemical synthesis
  • Sodium-Glucose Transporter 2 Inhibitors / chemistry
  • Sodium-Glucose Transporter 2 Inhibitors / pharmacology*
  • Structure-Activity Relationship


  • Glucosides
  • Hypoglycemic Agents
  • Sodium-Glucose Transporter 2
  • Sodium-Glucose Transporter 2 Inhibitors