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4(5)-Aryl-2-C-glucopyranosyl-imidazoles as New Nanomolar Glucose Analogue Inhibitors of Glycogen Phosphorylase.


ABSTRACT: Inhibition of glycogen phosphorylases may lead to pharmacological treatments of diseases in which glycogen metabolism plays an important role: first of all in diabetes, but also in cardiovascular and tumorous disorders. C-(?-d-Glucopyranosyl) isoxazole, pyrazole, thiazole, and imidazole type compounds were synthesized, and the latter showed the strongest inhibition against rabbit muscle glycogen phosphorylase b. Most efficient was 2-(?-d-glucopyranosyl)-4(5)-(2-naphthyl)-imidazole (11b, K i = 31 nM) representing the best nanomolar glucose derived inhibitor of the enzyme.

SUBMITTER: Bokor E 

PROVIDER: S-EPMC4677374 | biostudies-literature | 2015 Dec

REPOSITORIES: biostudies-literature

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4(5)-Aryl-2-C-glucopyranosyl-imidazoles as New Nanomolar Glucose Analogue Inhibitors of Glycogen Phosphorylase.

Bokor Éva É   Kun Sándor S   Docsa Tibor T   Gergely Pál P   Somsák László L  

ACS medicinal chemistry letters 20151019 12


Inhibition of glycogen phosphorylases may lead to pharmacological treatments of diseases in which glycogen metabolism plays an important role: first of all in diabetes, but also in cardiovascular and tumorous disorders. C-(β-d-Glucopyranosyl) isoxazole, pyrazole, thiazole, and imidazole type compounds were synthesized, and the latter showed the strongest inhibition against rabbit muscle glycogen phosphorylase b. Most efficient was 2-(β-d-glucopyranosyl)-4(5)-(2-naphthyl)-imidazole (11b, K i = 31  ...[more]

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