Synthesis of montbretin A analogues yields potent competitive inhibitors of human pancreatic alpha-amylase

Simplified analogues of the potent human amylase inhibitor montbretin A were synthesised and shown to bind tightly, K-I = 60 and 70 nM, with improved specificity over medically relevant glycosidases, making them promising candidates for controlling blood glucose. Crystallographic analysis confirmed similar binding modes and identified new active site interactions.