Diabetes mellitus is a medical condition characterized by the body's loss of control over blood sugar. The frequency of diagnosed cases and consequential increases in medical costs makes it a rapidly growing chronic disease that threatens human health worldwide. In addition, its unnerving statistical projections are perilous to both the economy of the nation and man's life expectancy. Type-I and type-II diabetes are the two clinical forms of diabetes mellitus. Type-II diabetes mellitus (T2DM) is illustrated by the abnormality of glucose homeostasis in the body, resulting in hyperglycemia. Although significant research attention has been devoted to the development of diabetes regimens, which demonstrates success in lowering blood glucose levels, their efficacies are unsustainable due to undesirable side effects such as weight gain and hypoglycemia. Over the years, heterocyclic scaffolds have been the basis of anti-diabetic chemotherapies; hence, in this review we consolidate the use of bioactive scaffolds, which have been evaluated for their biological response as inhibitors against their respective anti-diabetic molecular targets over the past five years (2012–2017). Our investigation reveals a diverse target set which includes; protein tyrosine phosphatase 1 B (PTP1B), dipeptidly peptidase-4 (DPP-4), free fatty acid receptors 1 (FFAR1), G protein-coupled receptors (GPCR), peroxisome proliferator activated receptor-γ (PPARγ), sodium glucose co-transporter-2 (SGLT2), α-glucosidase, aldose reductase, glycogen phosphorylase (GP), fructose-1,6-bisphosphatase (FBPase), glucagon receptor (GCGr) and phosphoenolpyruvate carboxykinase (PEPCK). This review offers a medium on which future drug design and development toward diabetes management may be modelled (i.e. optimization via structural derivatization), as many of the drug candidates highlighted show promise as an effective anti-diabetic chemotherapy.

糖尿病是以身体对血糖失去控制为特征的医学疾病。确诊病例的频度以及随之而来的医疗费用的增加，使其成为一种迅速增长的慢性病，​​威胁着全世界的人类健康。此外，其令人不安的统计预测对国家经济和人类预期寿命均有害。I型和II型糖尿病是糖尿病的两种临床形式。II型糖尿病（T2DM）由体内葡萄糖动态平衡异常引起，导致高血糖症。尽管人们对糖尿病治疗方案的开发投入了大量的研究注意力，这表明在降低血糖水平方面取得了成功，由于不良的副作用，例如体重增加和血糖过低，它们的功效难以为继。多年来，杂环支架一直是抗糖尿病化学疗法的基础。因此，在本综述中，我们巩固了生物活性支架的使用，这些支架在过去五年（2012-2017年）中作为其各自的抗糖尿病分子靶标的抑制剂已对其生物学反应进行了评估。我们的调查揭示了一个多样化的目标集，其中包括：蛋白酪氨酸磷酸酶1 B（PTP1B），二肽肽酶4（DPP-4），游离脂肪酸受体1（FFAR1），G蛋白偶联受体（GPCR），过氧化物酶体增殖物激活受体-γ（PPARγ），葡萄糖钠-transporter-2（SGLT2），α-葡萄糖苷酶，醛糖还原酶，糖原磷酸化酶（GP），果糖1,6-双磷酸酶（FBPase），胰高血糖素受体（GCGr）和磷酸烯醇丙酮酸羧激酶（PEPCK）。这篇综述提供了一种可以模拟未来药物设计和糖尿病治疗开发的媒介（例如通过结构衍生化进行优化），因为许多候选药物都显示出有望作为一种有效的抗糖尿病化学疗法。