The relationships between structures and inhibitory activities of glycosida
se inhibitors of gem-diamine 1-N-iminosugars in media of enzyme assays have
been investigated. It has been proved that gem-diamine 1-N-iminosugar smoo
thly undergoes a structural change to a hydrated ketone or its derivative v
ia a hemiaminal in the media (pH 5.0-6.3), and that the products generated
in the media as well as the parent gem-diamine 1-N-iminosugars potently inh
ibit glycosidases. (C) 2001 Elsevier Science Ltd. Al rights reserved.