Synthesis and biological evaluation of potent glycosidase inhibitors: N-phenyl cyclic isourea derivatives of 5-amino- and 5-amino-C-(hydroxymethyl)-1,2,3,4-cyclopentanetetraols

Add time:08/17/2019    Source:sciencedirect.com

Twenty-four stereoisomers of 5-amino- and 5-amino-C-(hydroxymethyl)-1,2,3,4-cyclopentanetetraols and twenty-six of the corresponding N-phenyl cyclic isourea derivatives were assayed for inhibitory activity against six glycosidases. Among them, as has been expected for structure mimics of putative transition state glucopyranosyl cation for glycoside hydrolysis, 1l-(1,2,4,53)-5-amino-1-C-(hydroxymethyl)-1,2,3,4-cyclopentanetetraoll-4 and its N-phenyl cyclic isourea derivative S-19 were shown to have strong inhibitory activity, IC50 4 × 10−7 and 7.6 × 10−9 M, respectively, against baker's yeast α-glucosidase. It has been analogously explained that compounds R,S-22 and R,S-26 possessed high inhibitory potency against Escherichia coli and bovine liver β-galactosidases, respectively.

We also recommend Trading Suppliers and Manufacturers of 1-((1,2,3,4)-2-Fluoro-3-hydroxy-4-( hydroxymethyl)cyclopentyl)-5-iodo- 2,4(1H,3H)-pyrimidinedione (cas 110864-93-2). Pls Click Website Link as below: cas 110864-93-2 suppliers

Prev:Original articleRole of genes GSTM1, GSTT1, and MnSOD in the development of late-onset Alzheimer disease and their relationship with APOE*4Papel de las variantes GSTM1, GSTT1 y MnSOD en el desarrollo de enfermedad de Alzheimer de aparición tardía y su relación con el alelo 4 de APOE☆
Next:Characterization of an acetan (cas 110865-71-9)-like heteropolysaccharide produced by Kozakia baliensis NBRC 16680)