芳香磺酰腙化合物的合成及其体外活性初筛-药物化学专业论文.docxVIP

汕头大 汕头大学医学院硕士研究生学位论文 PAGE PAGE VI ABSTRACT Hydrazones are special compounds in the Schiff base family that are characterized by the presence of a -NHN=C- group, and have been demonstrated to possess various bioactivity such as antioxidative, anti-inflammatory,antimicrobial, antiviral and antineoplastic activity.Also due to their strong abilities and multiplex patterns for coordination,hydrazones have caught high attention in fields of medicine,pesticide,materials science and analytic reagent. According to the theory of free radicals,excessive free radicals could cause and promote the development of diseases.Owing to the properties of hydrazones such as strong antioxidative ability and low toxicity, it may be a new direction for researchers to searching for effective anti-oxdants for clinical use from hydrazones. The dramatically increasing drug-resistance has prompted efforts to develop new classes of antibiotics, especially those can inhibit metallo-β-lactamase (MBLs).Due to the antibacterial activity and the coordinating capacity with metals,we hope to find new antibiotics from hydrazones, including MBLs inhibitors. On the basis of literature and previous investigations of our lab，in this work we want to systhesize a series of aromatic sulfonyl hydrazones and to test their antioxidative，antibacterial effect and inhibitating capacity on metallo-β-lactamase. Systhesis of sulfonyl hydrazones Methods:Using aromatic sulfonyl hydrazides and various aldehydes or ketones as materials, target compounds were systhesized by traditional nucleophilic addition and elimination reaction. Results: Eight aromatic sulfonyl hydrazone derivatives were synthesized and their structures were characterized by IR, 1H NMR, and MS techniques. Conclusions: A series of sulfonyl hydrazones have been prepared successfully. Study of in vitro scavenging capacity for free radical. Methods: Antioxidative potency of the target compounds was assessed in vitro by the DPPH assay. Hydroxy radical scav