Probing the aglycon binding site of a beta-glucosidase: a collection of C-1-modified 2,5-dideoxy-2,5-imino-d-mannitol derivatives and their structure-activity relationships as competitive inhibitors.

摘要

A range of new C-1 modified derivatives of the powerful glucosidase inhibitor 2,5-dideoxy-2,5-imino-d-mannitol has been synthesised and their biological activities probed with the beta-glucosidase from Agrobacterium sp. [Formula: see text] values are compared with those of previously prepared close relatives. Findings suggest dramatic effects exerted by the aglycon binding site on substrate/inhibitor binding.