Reference of 202189-78-4, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 202189-78-4, Name is Bilastine, SMILES is O=C(O)C(C)(C)C1=CC=C(CCN2CCC(C3=NC4=CC=CC=C4N3CCOCC)CC2)C=C1, belongs to indole-building-block compound. In a article, author is Wu, Panpan, introduce new discover of the category.
Oleanolic acid indole derivatives as novel alpha-glucosidase inhibitors: Synthesis, biological evaluation, and mechanistic analysis
Research efforts have been directed to the development of oleanolic acid (OA) based alpha-glucosidase inhibitors and various OA derivatives showed improved anti-alpha-glucosidase activity. However, the inhibitory effects of indole infused OA derivatives on alpha-glucosidase is unknown. Herein, we synthesized a series of indole-OA (2a-2o) and -OA methyl ester (3a-3 1) derivatives with various electron withdrawing groups inducted to indole benzene ring and evaluated their anti-alpha-glucosidase activity. Indole OA derivatives (2a-2o) exhibited superior alpha-glucosidase inhibitory effects as compared to OA methyl ester derivatives (3a-31) and OA (with IC50 values of 4.02 mu M-5.30 mu M v.s. over 10 mu M and 5.52 mu M, respectively). In addition, mechanistic studies using biochemical (kinetic assay), biophysical (circular dichroism), and computational (docking) methods revealed that OA-indole derivatives (2a and 2f) are mixed type of alpha-glucosidase inhibitors and their inhibitory effects were attributed to their capacity of forming the ligand-enzyme complex with alpha-glucosidase enzyme. Findings from this study support that OA indole derivatives are promising alpha-glucosidase inhibitors as a potential management of diabetes mellitus.
Reference of 202189-78-4, One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 202189-78-4.
Reference:
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