Department of Chemistry, University of Karachi, Karachi 75270, Pakistan.
Department of Chemistry and Earth Sciences, Qatar University, Doha, Qatar.
Med Chem. 2019;15(8):923-936. doi: 10.2174/1573406415666190213101044.
Antioxidant, anti-inflammatory, antiviral and antitumoral activities among others are essential characteristics in the development of novel therapeutic compounds. Acid hydrazides can form complexation with certain metal ions that positively enhance these biological characteristics.
Five new complexes of uranium with hydrazide ligands were synthesized at room temperature.
The characterization was done by spectroscopic methods (ESI-Mass, IR, 1H-NMR, 13CNMR), CHN analysis and conductivity measurements. Metal complexes along with their respective ligands were further screened for their antioxidant (DPPH, superoxide and nitric oxide free radicals) properties and enzyme inhibition (α-glucosidase) activities.
Elemental and spectral data indicate octahedral geometry around uranyl (UO2 2+) species. Magnetic moments indicate the diamagnetic nature of uranyl(VI) ion in the complex in solid state. IC50 values showed potential antioxidant behavior of uranyl complexes demonstrating interesting structure-activity relationships. In general, hydrazide ligands were not active against superoxide and nitric oxide radicals while varying degree of results were observed against DPPH radical whereas all uranyl-complexes showed promising radical scavenging activities against all of them. Promising inhibitory potential was displayed by UO2 +2 hydrazide complexes against α- glucosidases whereas free hydrazide ligands were inactive.
Structure function relationship demonstrates that the nature of ligand, position of substituent, electronic and steric effects are significant factors affecting the radical scavenging and enzyme inhibition activities of the compounds.
抗氧化、抗炎、抗病毒和抗肿瘤等活性是开发新型治疗化合物的重要特征。酸酰肼可以与某些金属离子形成配合物，从而积极增强这些生物特性。
在室温下合成了五个新的铀酰与酰肼配体的配合物。
通过光谱方法（ESI-Mass、IR、1H-NMR、13C-NMR）、CHN 分析和电导率测量进行了表征。金属配合物及其各自的配体进一步筛选了抗氧化（DPPH、超氧自由基和一氧化氮自由基）特性和酶抑制（α-葡萄糖苷酶）活性。
元素和光谱数据表明铀酰（UO22+）物种具有八面体几何形状。磁矩表明固态中铀酰（VI）离子具有抗磁性。IC50 值表明铀酰配合物具有潜在的抗氧化活性，表现出有趣的结构-活性关系。一般来说，酰肼配体对超氧自由基和一氧化氮自由基没有活性，而对 DPPH 自由基的活性则有所不同，而所有铀酰配合物对所有自由基都表现出有希望的自由基清除活性。UO2+2 酰肼配合物对α-葡萄糖苷酶表现出有希望的抑制潜力，而游离酰肼配体则没有活性。
结构-功能关系表明，配体的性质、取代基的位置、电子和空间效应是影响化合物自由基清除和酶抑制活性的重要因素。
