SGLT2 inhibitors, an accomplished development in field of medicinal chemistry: an extensive review

Future Med Chem. 2020 Nov;12(21):1961-1990. doi: 10.4155/fmc-2020-0154. Epub 2020 Oct 30.


Diabetes is a chronic progressive metabolic disease caused by insulin deficiency or insulin resistance. In spite of the availability of several antihyperglycaemics, there is a need for the development of safer antidiabetic drugs due to their undesirable effects. Sodium-glucose cotransporter-2 inhibitors are a class of antidiabetics, which hinder the reabsorption of glucose in the kidneys, causing excretion of glucose via urine. Sodium-glucose cotransporter-2 inhibitors are a well-tolerated class with no significant adverse effects and are found to be favorable in certain conditions, which may be rudimentary to cardiovascular and renal diseases. The current advancements in their design and development, their mechanism of action, structure-activity relationship, synthesis and in silico development along with their auxiliary roles have been extensively reviewed.

Keywords: SGLT2 inhibitors; antihyperglycemic drugs; diabetes; gliflozins; structure–activity relationship.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Chemistry, Pharmaceutical
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetes Mellitus, Type 2 / metabolism
  • Drug Development*
  • Humans
  • Molecular Conformation
  • Sodium-Glucose Transporter 2 / metabolism*
  • Sodium-Glucose Transporter 2 Inhibitors / chemical synthesis
  • Sodium-Glucose Transporter 2 Inhibitors / chemistry
  • Sodium-Glucose Transporter 2 Inhibitors / pharmacology*


  • SLC5A2 protein, human
  • Sodium-Glucose Transporter 2
  • Sodium-Glucose Transporter 2 Inhibitors