Abstract::
Diabetes mellitus is one of the biggest challenges for the scientific community in the 21st
century. With the increasing number of cases of diabetes and drug-resistant diabetes, there is an urgent
need to develop new potent molecules capable of combating this cruel disease. Medicinal
chemistry concerns the discovery, development, identification, and interpretation of the mode of
action of biologically active compounds at the molecular level. Oxadiazole-based derivatives have
come up as a potential option for antidiabetic drug research. Oxadiazole is a five-membered heterocyclic
organic compound containing two nitrogen atoms and one oxygen atom in its ring. Oxadiazole
hybrids have shown the ability to improve glucose tolerance, enhance insulin sensitivity, and
reduce fasting blood glucose levels. The mechanisms underlying the antidiabetic effects of oxadiazole
involve the modulation of molecular targets such as peroxisome proliferator-activated receptor
gamma (PPARγ), α-glucosidase, α-amylase and GSK-3β which regulate glucose metabolism and
insulin secretion. The present review article describes the chemical structure and properties of
oxadiazoles and highlights the antidiabetic activity through action on different targets. The SAR for
the oxadiazole hybrids has been discussed in this article, which will pave the way for the design and
development of new 1,3,4-oxadiazole derivatives as promising antidiabetic agents in the future. We
expect that this article will provide comprehensive knowledge and current innovation on oxadiazole
derivatives with antidiabetic potential and will fulfil the needs of the scientific community in designing
and developing efficacious antidiabetic agents.