Diabetes mellitus (DM) remains a global health concern, causing significant mortality and morbidity annually. Type-2 DM is the most prevalent and oral anti-diabetic drugs play a vital role in its management. There are several oral anti-diabetic drugs available in the market classified as sulfonylureas, thiazolidinediones, meglitinides, sodium glucose co-transporter (SGLT2), α-glucosidase inhibitors, dipeptidyl peptidase-(IV) inhibitors and biguanides. As the type-2 DM burden continues to surge, the scientific community has been working extensively towards the development of better and more sustainable synthetic strategies towards these anti-diabetics to prevent a potential public emergency. This review summaries various reported synthetic strategies for anti-diabetic drugs in the aforementioned classes. We envisage that this compilation will serve as an invaluable comprehensive foundation and reference source for the organic and medicinal chemists in the further development of DM drugs.

糖尿病 (DM) 仍然是一个全球性的健康问题，每年都会导致显着的死亡率和发病率。2 型糖尿病是最普遍的，口服抗糖尿病药物在其管理中起着至关重要的作用。市场上有几种口服抗糖尿病药物，分为磺脲类、噻唑烷二酮类、格列奈类、钠葡萄糖协同转运蛋白 (SGLT2)、α-葡萄糖苷酶抑制剂、二肽基肽酶 (IV) 抑制剂和双胍类。随着 2 型糖尿病负担持续激增，科学界一直致力于为这些抗糖尿病药物开发更好、更可持续的合成策略，以防止潜在的公共紧急情况。本综述总结了上述类别中各种已报道的抗糖尿病药物的合成策略。