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

2003; Wiley; Volume: 42; Issue: 38 Linguagem: Inglês

10.1002/anie.200351823

1521-3773

Chung‐Yi Wu, Chuan‐Fa Chang, Jenny Szu‐Yu Chen, Chi‐Huey Wong, Chun‐Hung Lin,

Legume Nitrogen Fixing Symbiosis

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.