Thioglycoligase-Based Assembly of Thiodisaccharides: Screening as β-Galactosidase Inhibitors

New way of doing things. An efficient inhibitor of a human lysosomal acid β‐galactosidase was identified through screening of a small collection of thioglycosides created by using a thioglycoligase derived from a bacterial β‐galactosidase (see scheme). The results described here open the interesting possibility of finding novel and unpredicted inhibitors of enzymes of interest through the relatively simple strategy of library generation by using thioglycoligases.