101908-41-2Relevant articles and documents
Synthesis and spectral characterisation of new amido-ether Schiff bases
Stamatoiu, Oana,Bubnov, Alexej,?arcomnicu, Isabela,Iovu, Mircea
, p. 187 - 196 (2008)
Series of new compounds prepared by condensing the sodium salt of 4-[(4-methoxy-benzylidene)-amino]-phenol with chloroacetanilides carrying various substituents in different positions has been synthesised and characterised by UV-VIS, FTIR, MS, 1H and 13C NMR spectrometry. The effect of type and position of different substituents on thermal and on mesomorphic behaviour has been investigated by polarizing optical microscopy and differential scanning calorimetry studies. All compounds possess relatively high phase transition temperatures due to possibility of forming molecular associations and only the 2,4-substituted ones possess the liquid crystalline behaviour, namely the nematic phase.
Design and synthesis of novel xanthone-triazole derivatives as potential antidiabetic agents: α-Glucosidase inhibition and glucose uptake promotion
Ye, Gao-Jie,Lan, Tian,Huang, Zhi-Xin,Cheng, Xiao-Ning,Cai, Chao-Yun,Ding, Sen-Miao,Xie, Min-Li,Wang, Bo
, p. 362 - 373 (2019/06/05)
Inhibiting the decomposition of carbohydrates into glucose or promoting glucose conversion is considered to be an effective treatment for type 2 diabetes. Herein, a series of novel xanthone-triazole derivatives were designed, synthesized, and their α-glucosidase inhibitory activities and glucose uptake in HepG2 cells were investigated. Most of the compounds showed better inhibitory activities than the parental compound a (1,3-dihydroxyxanthone, IC50 = 160.8 μM)and 1-deoxynojirimycin (positive control, IC50 = 59.5 μM)towards α-glucosidase. Compound 5e was the most potent inhibitor, with IC50 value of 2.06 μM. The kinetics of enzyme inhibition showed that compounds 5e, 5g, 5h, 6c, 6d, 6g and 6h were noncompetitive inhibitors, and molecular docking results were consistent with the noncompetitive property that these compounds bind to allosteric sites away from the active site (Asp214, Glu276 and Asp349). On the other hand, the glucose uptake assays exhibited that compounds 5e, 6a, 6c and 7g displayed high activities in promoting the glucose uptake. The cytotoxicity assays showed that most compounds were low-toxic to human normal hepatocyte cell line (LO2). These novel xanthone triazole derivatives exhibited dual therapeutic effects of α-glucosidase inhibition and glucose uptake promotion, thus they could be use as antidiabetic agents for developing novel drugs against type 2 diabetes.
GPR17 Receptor Modulators
-
Paragraph 0044; 0045, (2015/05/26)
Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases.
GPR17 RECEPTOR MODULATORS
-
Page/Page column 26-27, (2013/12/03)
The present invention relates to chemical compounds acting through GPR17 receptor for use in the treatment o f diseases, in particular for use in chronic and/or acute neurodegenerative diseases, preferably Multiple Sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, renal diseases.
