Synthesis and pharmacological evaluation of bis-3-(3,4-dichlorophenyl)acrylamide derivatives as glycogen phosphorylase inhibitors

2008 ◽  
Vol 16 (18) ◽  
pp. 8627-8634 ◽  
Author(s):  
Kenichi Onda ◽  
Ryota Shiraki ◽  
Yasuhiro Yonetoku ◽  
Kazuhiro Momose ◽  
Naoko Katayama ◽  
...  
Keyword(s):  
Glycogen Phosphorylase ◽  
Pharmacological Evaluation ◽  
Glycogen Phosphorylase Inhibitors

Phytogenic Polyphenols as Glycogen Phosphorylase Inhibitors: The Potential of Triterpenes and Flavonoids for Glycaemic Control in Type 2 Diabetes

2017 ◽  
Vol 24 (4) ◽  
pp. 384-403 ◽  
Author(s):  
Demetres Leonidas ◽  
Joseph Hayes ◽  
Atsushi Kato ◽  
Vassiliki Skamnaki ◽  
Demetra Chatzileontiadou ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Glycaemic Control ◽  
Glycogen Phosphorylase ◽  
Glycogen Phosphorylase Inhibitors

scholarly journals Crystallographic studies on acyl ureas, a new class of glycogen phosphorylase inhibitors, as potential antidiabetic drugs

2005 ◽  
Vol 14 (7) ◽  
pp. 1760-1771 ◽  
Author(s):  
Nikos G. Oikonomakos ◽  
Magda N. Kosmopoulou ◽  
Evangelia D. Chrysina ◽  
Demetres D. Leonidas ◽  
Ioannis D. Kostas ◽  
...  
Keyword(s):  
Glycogen Phosphorylase ◽  
Antidiabetic Drugs ◽  
New Class ◽  
Glycogen Phosphorylase Inhibitors

Glycogen phosphorylase inhibitors: a patent review (2008 – 2012)

2013 ◽  
Vol 23 (8) ◽  
pp. 1017-1032 ◽  
Author(s):  
Nicolas Gaboriaud-Kolar ◽  
Alexios-Leandros Skaltsounis
Keyword(s):  
Glycogen Phosphorylase ◽  
Patent Review ◽  
Glycogen Phosphorylase Inhibitors

Discovery and evaluation of novel benzazepinone derivatives as glycogen phosphorylase inhibitors with potent activity

2021 ◽  
pp. 00-00
Author(s):  
Youde Wang ◽  
Zhiwei Yan ◽  
Yachun Guo ◽  
Liying Zhang
Keyword(s):  
Glycogen Phosphorylase ◽  
Fasting Blood Glucose ◽  
Binding Mode ◽  
Rabbit Muscle ◽  
Fasting Blood Glucose Level ◽  
Docking Simulations ◽  
Key Enzyme ◽  
Glycogen Phosphorylase Inhibitors ◽  
Glycogen Catabolism

Glycogen phosphorylase (GP) is a key enzyme of glycogen catabolism, so it is significant to discover a new GP inhibitor. A series of benzazepinone derivatives were discovered as GP inhibitors with potent activity. Among these derivatives, compound 5d showed significant potential against rabbit muscle GPa (IC50 = 0.25 ± 0.05 μM) and cellular efficacy. The in vivo study revealed that 5d significantly inhibited increases in fasting blood glucose level in two kinds of hyperglycemic mice models. The possible binding mode of compound 5d was explored based on molecular docking simulations. These results indicated that derivatives with benzazepinone were potential chemical entities against hyperglycemia.

Thermodynamic Characterization of Allosteric Glycogen Phosphorylase Inhibitors

Biochemistry ◽  
2008 ◽  
Vol 47 (16) ◽  
pp. 4683-4691 ◽  
Author(s):  
Oliver Anderka ◽  
Petra Loenze ◽  
Thomas Klabunde ◽  
Matthias K. Dreyer ◽  
Elisabeth Defossa ◽  
...  
Keyword(s):  
Glycogen Phosphorylase ◽  
Thermodynamic Characterization ◽  
Glycogen Phosphorylase Inhibitors
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