791619-83-5Relevant articles and documents
Synthesis, in vitro and in silico screening of 2-amino-4-aryl-6-(phenylthio) pyridine-3,5-dicarbonitriles as novel α-glucosidase inhibitors
Ali, Muhammad,Faramarzi, Mohammad Ali,Jabbar, Abdul,Khan, Khalid Mohammed,Larijani, Bagher,Mahdavi, Mohammad,Perveen, Shahnaz,Salar, Uzma,Shamim, Shahbaz,Taha, Muhammad
, (2020/05/16)
Inhibition of α-glucosidase enzyme is of prime importance for the treatment of diabetes mellitus (DM). Apart of many organic scaffolds, pyridine based compounds have previously been reported for wide range of bioactivities. The current study reports a series of pyridine based synthetic analogues for their α-glucosidase inhibitory potential assessed by in vitro, kinetics and in silico studies. For this purpose, 2-amino-4-aryl-6-(phenylthio)pyridine-3,5-dicarbonitriles 1–28 were synthesized and subjected to in vitro screening. Several analogs, including 1–3, 7, 9, 11–14, and 16 showed many folds increased inhibitory potential in comparison to the standard acarbose (IC50 = 750 ± 10 μM). Interestingly, compound 7 (IC50 = 55.6 ± 0.3 μM) exhibited thirteen-folds greater inhibition strength than the standard acarbose. Kinetic studies on most potent molecule 7 revealed a competitive type inhibitory mechanism. In silico studies have been performed to examine the binding mode of ligand (compound 7) with the active site residues of α-glucosidase enzyme.
Heterogeneous Cu(II)/l-His@Fe3O4 nanocatalyst: A novel, efficient and magnetically-recoverable catalyst for organic transformations in green solvents
Norouzi, Masoomeh,Ghorbani-Choghamarani, Arash,Nikoorazm, Mohsen
, p. 92387 - 92401 (2016/10/11)
A novel, efficient and green Cu(ii)/l-His@Fe3O4 catalyst has been applied successfully in the synthesis of heterocyclic compounds. The resulting catalyst was used in the synthesis of 2,3-dihydroquinazolin-4(1H)-ones, polyhydroquinolines and 2-amino-6-(arylthio)pyridine-3,5-dicarbonitriles as biologically interesting compounds. The present research is focused on investigation of recycling, reusability and stability of the catalyst in phase reactions. The Cu(ii)/l-His@Fe3O4 catalyst was used at least six times with comparable activities to that of fresh catalyst. The chemical composition and the structure of the catalyst were analysed by TGA/DTG, EDS, XRD, VSM, FT-IR and SEM.
First report of multiple metal ions containing glass-ceramic material as a heterogeneous ditopic catalyst for the chromatography free synthesis of 2-amino-3,5-dicarbonitrile-6-arylthio-pyridines in water
Manna, Priyabrata,Maiti
supporting information, p. 5094 - 5098 (2015/08/06)
This is the first report of the use of multiple metal ions containing glass-ceramic material as a reusable heterogeneous catalyst for multicomponent organic synthesis. A new glass-ceramic material was prepared for this purpose and applied in the sustainab