Diabetes mellitus (DM) is a major metabolic disorder due to hyperglycemia, which is increasing all over the world. From the last two decades, the use of synthetic agents has risen due to their major involvement in curing of chronic diseases including DM. The core skeleton of drugs has been studied such as thiazolidinone, azole, chalcone, pyrrole and pyrimidine along with their derivatives. Diabetics assays have been performed in consideration of different enzymes such as α-glycosidase, α-amylase, and α-galactosidase against acarbose standard drug. The studied moieties were depicted in both models: in vivo as well as in vitro. Molecular docking of the studied compounds as antidiabetic molecules was performed with the help of Auto Dock and molecular operating environment (MOE) software. Amino acid residues Asp349, Arg312, Arg439, Asn241, Val303, Glu304, Phe158, His103, Lys422 and Thr207 that are present on the active sites of diabetic related enzymes showed interactions with ligand molecules. In this review data were organized for the synthesis of heterocyclic compounds through various routes along with their antidiabetic potential, and further studies such as pharmacokinetic and toxicology studies should be executed before going for clinical trials.