214784-10-8Relevant academic research and scientific papers
N-benzylgalactonoamidines as potent β-galactosidase inhibitors
Kanso, Rami,Yancey, Elizabeth A.,Striegler, Susanne
scheme or table, p. 47 - 52 (2012/01/05)
A series of N-benzylgalactonoamidines was synthesized to probe their inhibitory ability during the hydrolysis of o-nitrophenyl-β-d- galactopyranoside by β-galactosidase (Aspergillus oryzae). All compounds are characterized as potent competitive inhibitors with inhibition constants (Ki) in the low nanomolar range (12-48 nM). The structure of the inhibitors mimics the bond-lengthening during the hydrolysis and the aromatic aglycon of the substrate. The electronic nature of the substituent in p-position of the aglycon influences the overall inhibitory ability most when compared to the unsubstituted parent compound.
Multi gram-scale synthesis of galactothionolactam and its transformation into a galactonoamidine
Kanso, Rami,Striegler, Susanne
experimental part, p. 897 - 904 (2011/06/19)
We recently proposed to conduct selective glycosylation reactions after in situ activation of a glycosyl donor promoted by a transition metal complex immobilized in a macromolecular matrix. In order to develop this catalytic entity, a feasible multi gram-
Inhibition of Glycosidases by Lactam Oximes: Influence of the Aglycon in Disaccharide Analogues
Vonhoff, Stefan,Heightman, Tom D.,Vasella, Andrea
, p. 1710 - 1725 (2007/10/03)
The influence of a substituent at the hydroximo function of the lactam analogue 1 on the inhibition of β- and α-glucosidases is evaluated. In contrast to 1, the O-alkyl oximes 5, 6, 9, and 10 are selective inhibitors of β-glucosidases. Alkylation of the D
