| Popis: |
Here, we demonstrate on the design and synthesis of novel pyrazine containing 1,2,3-triazole derivatives (, , and ) using various chemicals, bases, and catalysts synthesized with excellent yields (78–92%) as described in the procedures. The development of this methodology is simple, efficient, and easier to handle; milder reaction conditions and higher selectivity under versatile coupling reagent useful for both amide and ester bond formations have also been developed. The synthesis of amide coupling derivatives prepared by () was coupled with N-ethylpiperazine to afford () and morpholine to afford () by using 1-[Bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxid hexafluorophosphate (HATU) and N,N-diisopropylethylamine (DIPEA) in dichloromethane at room temperature for 10 h. The derivatives () were coupled with alcohol () by using N,N′-dicyclohexylcarbodiimide and 4-dimethylaminopyridine in dichloromethane (DCM) at room temperature for 16 h to give final compounds (). In silico docking approach has been applied to these compounds to screen their efficacy against selected drug targets of cancer and diabetes. The docking approach may facilitate the prediction of activity profile for future experimental findings. |
Plný text