Rapid Diversity‐Oriented Synthesis in Microtiter Plates for In Situ Screening: Discovery of Potent and Selective α‐Fucosidase Inhibitors

An efficient and simple method has been developed to identify potent and selective inhibitors against α-fucosidases based on the amide-forming reaction in a microtiter plate of a fuconojirimycin core with various carboxylic acids, followed by a direct inhibition assay without product isolation. The structures of the two most potent inhibitors are shown.