Synthetic and Crystallographic Insight into Exploiting sp(2) Hybridization in the Development of α‐l‐Fucosidase Inhibitors

The sugar fucose plays a myriad of roles in biological recognition. Enzymes hydrolyzing fucose from glycoconjugates, α‐l‐fucosidases, are important targets for inhibitor and probe development. Here we describe the synthesis and evaluation of novel α‐l‐fucosidase inhibitors, with X‐ray crystallographic analysis using an α‐l‐fucosidase from Bacteroides thetaiotamicron helping to lay a foundation for future development of inhibitors for this important enzyme class.