Wang, Youde; Yan, Zhiwei; Guo, Yachun; Zhang, Liying published the artcile< Discovery and evaluation of novel benzazepinone derivatives as glycogen phosphorylase inhibitors with potent activity>, Recommanded Product: 5-Fluoroindole-2-carboxylic acid, the main research area is benzazepinone derivative glycogen phosphorylase inhibitor hyperglycemia; benzazepinone derivatives; biological activity; glycogen phosphorylase inhibitors; molecular docking; type 2 diabetes.
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 mol. docking simulations. These results indicated that derivatives with benzazepinone were potential chem. entities against hyperglycemia.
Future Medicinal Chemistry published new progress about Absorption. 399-76-8 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Recommanded Product: 5-Fluoroindole-2-carboxylic acid.
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles