In this study, bornyl- and cytisine-based cyanopyrrolidines as potent dipeptidyl peptidase-IV (DPP-IV) inhibitors were synthesised. The in vitro inhibiting activities of bornyl- and cytisine derivatives towards DPP-IV were evaluated. Bornyl-based cyanopyrrolidines were shown to have moderate inhibitory activity with regard to DPP-IV (1.27–15.78 µM). A docking study was performed to elucidate the structure-activity relationship of the obtained compounds. The in vivo hypoglycemic activities of the same compounds were evaluated with the oral glucose tolerance test (OGTT) in mice. Bornyl-based cyanopyrrolidines were shown to have good hypoglycemic activity.

在这项研究中，合成了基于冰片和胱氨酸的氰基吡咯烷类作为有效的二肽基肽酶-IV（DPP-IV）抑制剂。在体外bornyl-并朝向DPP-IV金雀花碱衍生物的抑制活性进行了评价。已显示基于硼烷基的氰基吡咯烷对DPP-IV具有中等抑制活性（1.27–15.78 µM）。进行对接研究以阐明获得的化合物的结构-活性关系。在体内的相同化合物的降血糖活性用小鼠口服葡萄糖耐量试验（OGTT）进行评价。证实基于硼烷基的氰基吡咯烷具有良好的降血糖活性。