| Pyridinium salts have versatile chemical reactivity beacuse of the aromatic character of the pyridine heterocycle, its basicity and the electro-attracting influence of the nitrogen atom in pyridine. They have various synthesis methods in organic synthesis. Nitrogen heterocycles can be used to synthesis natural products and biologically active compounds. Pyridinium salts are nitrogen heterocycles, which are widely used in biology, medicine, chemistry and other fields.Thirty-two novel 2-amino-1-[3-oxo-3-(substituted-anline)propyl]pyridinium nitrate bearing hydrogen, methyl, methoxy, fluorine, chlorine are designed and prepared via one-pot tandem reactions using 2-aminopyridine and ethyl acrylate as raw materials in this study. Their structures were elucidated by 1H NMR, 13C NMR and HR-MS. The compound crystal structures were cultured and tested by X-ray crystallographic analysis to further determine the structure if 2-amino-1-[3-oxo-(substituted-aniline)propyl]pyridinium. A potential mechanism is speculated.The substituent-reaction activity relationship of anilines with different substituents (i.e., H, CH3,OCH3, F, and Cl) and different substituted positions in pyridinium nitrate was summarized based on the reaction results.Besides, on the basis of our former synthesis of resveratrol derivatives, the anticoagulant activity of resveratrol derivatives was studied. Twenty-five resveratrol heterocyclic derivatives were evaluated for thrombin activity in vitro, four compounds showed better thrombin inhibitory activity with IC50 values 10.43, 10.90,17.72, 18.31 ?M than resveratrol(IC50=25.87?M). Especially, compounds 4d and 4j may be potential candidate to further research for the prevention and treatment of cardiovascular diseases. |
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