1171243-26-7Relevant articles and documents
Synthesis, molecular docking and α-glucosidase inhibition of 5-aryl-2-(6′-nitrobenzofuran-2′-yl)-1,3,4-oxadiazoles
Taha, Muhammad,Ismail, Nor Hadiani,Imran, Syahrul,Wadood, Abdul,Rahim, Fazal,Saad, Syed Muhammad,Khan, Khalid Mohammed,Nasir, Abdul
, p. 117 - 123 (2016)
Twenty derivatives of 5-aryl-2-(6′-nitrobenzofuran-2′-yl)-1,3,4-oxadiazoles (1–20) were synthesized and evaluated for their α-glucosidase inhibitory activities. Compounds containing hydroxyl and halogens (1–6, and 8–18) were found to be five to seventy folds more active with IC50 values in the range of 12.75?±?0.10–162.05?±?1.65?μM, in comparison with the standard drug, acarbose (IC50?=?856.45?±?5.60?μM). Current study explores the α-glucosidase inhibition of a hybrid class of compounds of oxadiazole and benzofurans. These findings may invite researchers to work in the area of treatment of hyperglycemia. Docking studies showed that most compounds are interacting with important amino acids Glu 276, Asp 214 and Phe 177 through hydrogen bonds and arene-arene interaction.
Highly efficient copper/palladium-catalyzed tandem Ullman reaction/arylation of azoles via C-H activation: Synthesis of benzofuranyl and indolyl azoles from 2-(gem-dibromovinyl)phenols(anilines) with azoles
Chen, Wei,Wang, Min,Li, Pinhua,Wang, Lei
experimental part, p. 5913 - 5919 (2011/09/19)
In this paper, a novel and highly efficient copper/palladium-catalyzed tandem intramolecular Ullman-type C-O(N) coupling reaction of 2-(gem-dibromovinyl)phenols(anilines) followed by an intermolecular arylation of azoles through C-H activation has been developed. In the presence of CuBr with Pd(PPh3)2Cl2 used as co-catalyst, and LiO tBu as a base, the one-pot reactions of 2-(gem-dibromovinyl)phenols and 2-(gem-dibromovinyl)anilines with a variety of azoles, including oxazoles, imidazoles, thiazoles, and oxadiazoles underwent smoothly in toluene at 100 °C to generate the corresponding biheteroaryl products in high yields. A tentative mechanism of copper/palladium-catalyzed tandem reaction was described.