1137-99-1Relevant academic research and scientific papers
Design and synthesis of tricyclic terpenoid derivatives as novel PTP1B inhibitors with improved pharmacological property and in vivo antihyperglycaemic efficacy
Chen, Feng,Chen, Jiabao,Gao, Cheng,Li, Junyan,Liu, Siyan,Qian, Shan,Wang, Zhouyu,Yang, Lingling,Zhang, Yuanyuan
, p. 152 - 164 (2019/11/25)
Overexpression of protein tyrosine phosphatase 1B (PTP1B) induces insulin resistance in various basic and clinical research. In our previous work, a synthetic oleanolic acid (OA) derivative C10a with PTP1B inhibitory activity has been reported. However, C10a has some pharmacological defects and cytotoxicity. Herein, a structure-based drug design approach was used based on the structure of C10a to elaborate the smaller tricyclic core. A series of tricyclic derivatives were synthesised and the compounds 15, 28 and 34 exhibited the most PTP1B enzymatic inhibitory potency. In the insulin-resistant human hepatoma HepG2 cells, compound 25 with the moderate PTP1B inhibition and preferable pharmaceutical properties can significantly increase insulin-stimulated glucose uptake and showed the insulin resistance ameliorating effect. Moreover, 25 showed the improved in vivo antihyperglycaemic potential in the nicotinamide–streptozotocin-induced T2D. Our study demonstrated that these tricyclic derivatives with improved molecular architectures and antihyperglycaemic activity could be developed in the treatment of T2D.
PROCESS FOR PREPARING BIS(2-HYDROXYETHYL) TEREPHTHALATE
-
Paragraph 0025-0036, (2020/01/04)
A process for preparing bis(2-hydroxyethyl) terephthalate, comprising a step of: subjecting ethylene oxide and terephthalic acid in a molar ratio of from 2.5:1 to 3.5:1 to a reaction at an elevated temperature of up to 150° C. in the presence of a solvent mixture containing water and a diol cosolvent in a weight ratio of from 0.2:1 to 5:1.
Bis (2 - hydroxyethyl) (2 - hydroxyethyl) terephthalate and glycosylation of terephthalic acid mono-glycosylated
-
Paragraph 0061; 0062; 0063; 0064; 0065; 0066; 0067; 0068, (2019/08/16)
The invention concerns a compound characterised by a mono(2-hydroxyethyl) terephthalic acid (MHET) and bis(2-hydroxyethyl) terephthalic acid chemically bonded to a saccharide. Furthermore, the invention concerns a corresponding compound which is used as a
