Thio-β-D-glucosides: Synthesis and Evaluation as Glycosidase Inhibitors and Activators

Structurally simple 1-thio-β-D-glucopyranosides were synthesized and tested as potential inhibitors toward several fungal glycosidases from Aspergillus oryzae and Penicillium canescens. Significant selective inhibition was observed for α- and β-glucosidases, while a weak to moderate activation for α- and β-galactosidases.

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Prediction of selective inhibition of neuraminidase from various influenza virus strains by potential inhibitors

Biochemistry (Moscow) Supplement Series B Biomedical Chemistry ◽

10.1134/s1990750817020044 ◽

2017 ◽

Vol 11 (2) ◽

pp. 166-185

Author(s):

A. V. Mikurova ◽

A. V. Rybina ◽

V. S. Skvortsov

Keyword(s):

Influenza Virus ◽

Selective Inhibition ◽

Potential Inhibitors ◽

Virus Strains

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Prediction of selective inhibition of neuraminidase from various influenza virus strains by potential inhibitors

Biomeditsinskaya Khimiya ◽

10.18097/pbmc20166206691 ◽

2016 ◽

Vol 62 (6) ◽

pp. 691-703 ◽

Cited By ~ 6

Author(s):

A.V. Mikurova ◽

A.V. Rybina ◽

V.S. Skvortsov

Keyword(s):

Influenza Virus ◽

3D Structure ◽

Selective Inhibition ◽

Regression Equations ◽

Independent Variables ◽

3D Data ◽

Ic50 Values ◽

Potential Inhibitors ◽

Virus Strains ◽

Selection Of

A universal model of inhibition of neuraminidases from various influenza virus strains by a particular has been developed. It is based on known 3D data for neuraminidases from three influenza virus strains (A/Tokyo/3/67, A/tern/Australia/G70C/75, B/Lee/40) and modeling of 3D structure of neuraminidases from other strains (A/PR/8/34 and A/Aichi/2/68). Using docking and molecular dynamics, we have modeled 235 enzyme-ligand complexes for 185 compounds with known IC50 values. Selection of final variants among three results obtained for each enzyme-ligand pair and calculation of independent variables for generation of linear regression equations was performed using MM-PBSA/MM-GBSA. This resulted in the set of equations individual strains and the equations pooling all the data. Thus using this approach it is possible to predict inhibition for neuraminidase from each of the considered strains by a particular inhibitor and to predict the range of its action on neuraminidases from various influenza virus strains.

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Selective Inhibition of Intestinal Disaccharide Absorption by Deoxynojirimycin-Derived Glycosidase Inhibitors

Clinical Science ◽

10.1042/cs067041pb ◽

1984 ◽

Vol 67 (s9) ◽

pp. 41P-42P

Author(s):

Rodney H. Taylor ◽

Helen M. Barker ◽

Elizabeth A. Bowey ◽

Jean E. Canfield

Keyword(s):

Selective Inhibition ◽

Glycosidase Inhibitors

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Synthesis and evaluation of galacto-noeurostegine and its 2-deoxy analogue as glycosidase inhibitors

Organic & Biomolecular Chemistry ◽

10.1039/c5ob01062d ◽

2015 ◽

Vol 13 (29) ◽

pp. 7979-7992 ◽

Cited By ~ 5

Author(s):

Stéphane Salamone ◽

Lise L. Clement ◽

Agnete H. Viuff ◽

Ole Juul Andersen ◽

Frank Jensen ◽

...

Keyword(s):

Aspergillus Oryzae ◽

Glycosidase Inhibitors ◽

Glycosidase Inhibitor

An epimer of the known glycosidase inhibitor noeurostegine, galacto-noeurostegine, was synthesised in 21 steps from levoglucosan and found to be a potent, competitive and highly selective galactosidase inhibitor of Aspergillus oryzae β-galactosidase.

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