Diabetes mellitus is the global health issue and become an alarming threat in 
the modern era where human lifestyle gets compromised with modernization. 
According to the latest statistical report 2020, USA has 9.47% (31 million among 
32.72 cr), China has 8.3% (116.4 million among 139.27 cr) and India has 5.6% (77 
million among 135.26 cr) of the diabetic people, indicating that diabetes is 
more prevailing in developed countries as compared to the developing countries. 
The number of diabetic patients is rising day by day at a tremendous rate and 
soon it may affect each and every person in a family. So, there is an urgent 
need to develop novel entities that can meet the scarcity of present 
antidiabetic agents. In the last few decades, the sodium-glucose co-transporter 
2 (SGLT2) has emerged as a prominent target for the treatment of Type 2 diabetes 
mellitus due to its novel mechanism of action & no involvement in insulin 
signaling pathway. Most of the inhibitors that target SGLT2 contain three basic 
moieties: glucose, two benzene rings (one is connected with glucose and the 
other with methylene), and the methylene bridge which are similar to 
dapagliflozin. Several SGLT2 inhibitors and their derivatives such as 
remogliflozin etabonate (phase-II), sotagliflozin (phase-III) and bexagliflozin 
(phase-III) are under different phases of clinical trial studies and some have 
been patented. The present review is focused on SGLT2 inhibitors, structure 
activity relationships (SARs) of dapagliflozin and its several analogues for 
their binding affinity with SGLT2. We have also presented and summarized the 
efforts made by various researchers in terms of the synthesis of various 
dapagliflozin derivatives till date.