Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 392-56-3, Name is Hexafluorobenzene, molecular formula is C6F6, belongs to benzoxazole compound, is a common compound. In a patnet, author is Wang, Mei-Yan, once mentioned the new application about 392-56-3, Quality Control of Hexafluorobenzene.
Synthesis and biological evaluation of novel N-aryl-omega-(benzoazol-2-yl)-sulfanylalkanamides as dual inhibitors of alpha-glucosidase and protein tyrosine phosphatase 1B
alpha-Glucosidase is known to catalyze the digestion of carbohydrates and release free glucose into the digestive tract. Protein tyrosine phosphatase 1B (PTP1B) is engaged in the dephosphorylation of the insulin receptor and regulation of insulin sensitivity. Therefore, dual antagonists by targeting both -glucosidase and PTP1B may be potential candidates for type 2 diabetes therapy. In this work, three series of novel N-aryl–(benzoazol-2-yl)-sulfanylalkanamides were synthesized and assayed for their -glucosidase and PTP1B inhibitory activities, respectively. Compound 3l, exhibiting the most effective -glucosidase inhibitory activity (IC50=10.96m (3l), IC50=51.32m (Acarbose), IC50=18.22m (Ursolic acid)) and potent PTP1B inhibitory activity (IC50=13.46m (3l), IC50=14.50m (Ursolic acid)), was identified as a novel dual inhibitor of -glucosidase and PTP1B. Furthermore, 3l is a highly selective PTP1B inhibitor because no inhibition was showed by 3l at 100m against PTP-MEG2, TCPTP, SHP2, or SHP1. Subsequent kinetic analysis revealed 3l inhibited -glucosidase in a reversible and mixed manner. Molecular docking study indicated that hydrogen bonds, van der Waals, charge interactions and Pi-cation interactions all contributed to affinity between 3l and -glucosidase/PTP1B.
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Reference:
Benzoxazole – Wikipedia,
,Benzoxazole | C7H5NO – PubChem