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Bokor É, Kun S, Docsa T, et al. 4(5)-Aryl-2-C-glucopyranosyl-imidazoles as New Nanomolar Glucose Analogue Inhibitors of Glycogen Phosphorylase. ACS Med Chem Lett. 2015;6(12):1215-9doi: 10.1021/acsmedchemlett.5b00361.
Bokor, �. �., Kun, S., Docsa, T., Gergely, P., & Somsák, L. (2015). 4(5)-Aryl-2-C-glucopyranosyl-imidazoles as New Nanomolar Glucose Analogue Inhibitors of Glycogen Phosphorylase. ACS medicinal chemistry letters, 6(12), 1215-9. https://doi.org/10.1021/acsmedchemlett.5b00361
Bokor, Éva, et al. "4(5)-Aryl-2-C-glucopyranosyl-imidazoles as New Nanomolar Glucose Analogue Inhibitors of Glycogen Phosphorylase." ACS medicinal chemistry letters vol. 6,12 (2015): 1215-9. doi: https://doi.org/10.1021/acsmedchemlett.5b00361
Bokor É, Kun S, Docsa T, Gergely P, Somsák L. 4(5)-Aryl-2-C-glucopyranosyl-imidazoles as New Nanomolar Glucose Analogue Inhibitors of Glycogen Phosphorylase. ACS Med Chem Lett. 2015 Oct 19;6(12):1215-9. doi: 10.1021/acsmedchemlett.5b00361. eCollection 2015 Dec 10. PMID: 26713107; PMCID: PMC4677374.
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ACS Med Chem Lett. 2015 Oct 19;6(12):1215-9. doi: 10.1021/acsmedchemlett.5b00361. eCollection 2015 Dec 10.

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

ACS medicinal chemistry letters

Éva Bokor, Sándor Kun, Tibor Docsa, Pál Gergely, László Somsák

Affiliations

  1. Department of Organic Chemistry, University of Debrecen , POB 20, H-4010 Debrecen, Hungary.
  2. Department of Medical Chemistry, Faculty of Medicine, University of Debrecen , Egyetem tér 1, H-4032 Debrecen, Hungary.

PMID: 26713107 PMCID: PMC4677374 DOI: 10.1021/acsmedchemlett.5b00361

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-(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 nM) representing the best nanomolar glucose derived inhibitor of the enzyme.

Keywords: C-Glucopyranosyl derivative; glycogen phosphorylase; imidazole; inhibitor; isoxazole; pyrazole; thiazole

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