Synthesis, pharmacological evaluation and structure-activity relationship of recently discovered enzyme antagonist azoles

A Dorababu - Heliyon, 2020 - cell.com
Global people are suffering from the legion of diseases. Cytotoxic property of the chemical
compound would not solely influence effective drug properties and reduce unnecessary side …

Metformin and Berberine suppress glycogenolysis by inhibiting glycogen phosphorylase and stabilizing the molecular structure of glycogen in db/db mice

X Liu, K Wang, J Zhou, MA Sullivan, Y Liu… - Carbohydrate …, 2020 - Elsevier
Glycogen is a branched glucose polymer involved in sustaining blood glucose homeostasis.
Liver glycogen comprises α particles (up to 300 nm in diameter) made of joined β particles …

[HTML][HTML] Nanomolar inhibition of human OGA by 2-acetamido-2-deoxy-d-glucono-1, 5-lactone semicarbazone derivatives

M Kiss, E Szabó, B Bocska, LT Sinh… - European Journal of …, 2021 - Elsevier
O-GlcNAcylation is a dynamic post-translational modification mediated by O-linked β-N-
acetylglucosamine transferase (OGT) and O-GlcNAc hydrolase (OGA), that adds or removes …

Dual-Target Compounds against Type 2 Diabetes Mellitus: Proof of Concept for Sodium Dependent Glucose Transporter (SGLT) and Glycogen Phosphorylase (GP) …

Á Sipos, E Szennyes, NÉ Hajnal, S Kun, KE Szabó… - Pharmaceuticals, 2021 - mdpi.com
A current trend in the quest for new therapies for complex, multifactorial diseases, such as
diabetes mellitus (DM), is to find dual or even multi-target inhibitors. In DM, the sodium …

In Silico-Motivated Discovery of Novel Potent Glycogen Synthase-3 Inhibitors: 1-(Alkyl/arylamino)-3H-naphtho[1,2,3-de]quinoline-2,7-dione Identified as a Scaffold for …

TD Emmerich, JM Hayes - Pharmaceuticals, 2023 - mdpi.com
Glycogen synthase kinase-3 (GSK-3) isoforms α and β have diverse roles within cell biology,
and have been linked with multiple diseases that include prominent CNS conditions such as …

Nickel and Chiral Phosphoric Acid Cocatalysis Enables Synthesis of C-Acyl Glycosides

L Zhang, W Zeng, D Xie, J Li, X Ma - Organic Letters, 2024 - ACS Publications
We disclosed a Ni/CPA cocatalyzed protocol to access diverse C-acyl glycosides under mild
conditions with broad functional group compatibility through the coupling of readily available …

Synthesis, In Silico and Kinetics Evaluation of N-(β-d-glucopyranosyl)-2-arylimidazole-4(5)-carboxamides and N-(β-d-glucopyranosyl)-4(5)-arylimidazole-2 …

L Homolya, RT Mathomes, L Varga, T Docsa… - International Journal of …, 2024 - mdpi.com
Recently studied N-(β-d-glucopyranosyl)-3-aryl-1, 2, 4-triazole-5-carboxamides have proven
to be low micromolar inhibitors of glycogen phosphorylase (GP), a validated target for the …

N-and C-Glycopyranosyl heterocycles as glycogen phosphorylase inhibitors

É Bokor - Recent Trends in Carbohydrate Chemistry, 2020 - Elsevier
Glycogen phosphorylase (GP), the main regulatory enzyme of glycogen degradation directly
controlling blood sugar levels, is a validated target in seeking new therapies against type 2 …

ZG02 improved hepatic glucose metabolism and insulin sensitivity via activation of AMPK/Sirt1 signaling pathways in a high-fat diet/streptozotocin-induced type 2 …

Y Zhang, B Zhou, M Wen, M Hu, JG Peng… - Diabetes, Metabolic …, 2020 - Taylor & Francis
Purpose The aim of the present study was to investigate the hypoglycemic activity and
potential mechanism of tetrahydrocarbazole derivatives ZG02 in high-fat diet/streptozotocin …

The architecture of hydrogen and sulfur σ-hole interactions explain differences in the inhibitory potency of C-β-d-glucopyranosyl thiazoles, imidazoles and an N-β-d …

E Kyriakis, AG Karra, O Papaioannou, T Solovou… - Bioorganic & Medicinal …, 2020 - Elsevier
C-Glucopyranosyl imidazoles, thiazoles, and an N-glucopyranosyl tetrazole were assessed
in vitro and ex vivo for their inhibitory efficiency against isoforms of glycogen phosphorylase …