The rising incidence of diabetes and confines allied with clinical therapies emphasized the need to explore new molecular targets to develop novel, effective and safer antihyperglycemic agents. Excessive endogenous glucose production by gluconeogenesis is a primary determinant of hyperglycemia in patients with type 2 diabetes. But not even a single current medication acts directly to reduce gluconeogenesis. Fructose-1,6-bisphosphatase (FBPase), a well recognized rate controlling enzyme of gluconeogenesis, has emerged as legitimate molecular level target to control gluconeogenesis mediated glucose overproduction and its inhibitors are likely to fulfill an unmet medical need. In this compilation various chemical classes of FBPase inhibitors have been reviewed which mainly acts through uncompetitive and non-competitive manner. A detailed account on structure activity relationship studies of inhibitors have been presented along with their molecular level interactions at binding sites of enzyme. Three Dimensional Quantitative Structure Activity relationship (3D-QSAR) studies, performed to optimize the lead, have been summarized at some places. In this assemblage, FBPase inhibitors patented in past have been compiled in tabular form. This review highlights the new insight into the therapeutic utility of FBPase inhibitors and their potential as a new class of antidiabetic drugs.

糖尿病的发病率上升以及与临床疗法相关的局限性强调了探索新的分子靶标以开发新型，有效和安全的降血糖药的必要性。糖异生作用导致的过多内源性葡萄糖产生是2型糖尿病患者高血糖的主要决定因素。但是，甚至没有一种目前的药物能直接起到减少糖异生的作用。果糖-1,6-双磷酸酶（FBPase）是公认的糖异生率控制酶，已成为控制糖异生介导的葡萄糖超量生产的合法分子水平靶标，其抑制剂可能满足未满足的医学需求。在本汇编中，对FBPase抑制剂的各种化学类别进行了综述，它们主要通过非竞争性和非竞争性方式发挥作用。已经提出了关于抑制剂的结构活性关系研究的详细说明，以及它们在酶结合位点的分子水平相互作用。在某些地方，对为优化铅而进行的三维定量结构活度关系（3D-QSAR）研究进行了总结。在这种组合中，过去获得专利的FBPase抑制剂已制成表格形式。这篇综述强调了对FBPase抑制剂的治疗作用及其作为一类新型抗糖尿病药的潜力的新见解。在这种组合中，过去获得专利的FBPase抑制剂已制成表格形式。这篇综述强调了对FBPase抑制剂的治疗作用及其作为一类新型抗糖尿病药的潜力的新见解。在这种组合中，过去获得专利的FBPase抑制剂已制成表格形式。这篇综述强调了对FBPase抑制剂的治疗作用及其作为一类新型抗糖尿病药的潜力的新见解。