论文部分内容阅读
为了探索新型高效脲酶抑制剂,本文合成了2个新的酰腙氧钒(V)配合物,[VOL1(OCH3)(CH3OH)](1)和[VOL2(μ-OCH3)]2(2)(H2L1=N′-(5-氯-2-羟基苯亚甲基)-3-硝基苯甲酰肼;H2L2=N′-(5-氯-2-羟基苯亚甲基)-4-氯苯甲酰肼),并通过物理化学方法和单晶X-射线衍射表征了它们的结构。化合物1是一个单核配合物,而化合物2是由两个甲氧基配体桥连的具有中心对称性的双核配合物。在每个配合物中,V原子都采取八面体配位构型。本文还研究了这两个配合物的热稳定性和它们对幽门螺旋杆菌脲酶的抑制活性。在浓度为100μmol.L-1时,配合物1和2对脲酶的抑制率分别为71.4%和73.3%,其IC50值分别为63.6和37.7μmol.L-1。
In order to explore a novel and highly efficient urease inhibitor, two new complexes of [VOH (VCH) (CH3OH)] and [VOL2 (μ-OCH3) (H2L1 = N’- (5-chloro-2-hydroxybenzylidene) -3-nitrobenzohydrazide; H2L2 = N’- (5-chloro-2- hydroxybenzylidene) -4- Chlorobenzohydrazide), and their structures were characterized by physicochemical methods and single crystal X-ray diffraction. Compound 1 is a mononuclear complex, while compound 2 is a centrally symmetrical binuclear complex bridged by two methoxy ligands. In each complex, V atoms adopt octahedral coordination configuration. We also studied the thermal stability of these two complexes and their inhibitory activity against H. pylori urease. The inhibitory rates of complex 1 and 2 on urease were 71.4% and 73.3%, respectively, with IC50 values of 63.6 and 37.7 μmol·L-1, respectively, at a concentration of 100 μmol·L-1.