【作者】 赵海峰；

【导师】 王麟生；

【作者基本信息】 华东师范大学 ， 无机化学， 2005， 硕士

【摘要】 杂环缩氨基硫脲具有良好的生物活性。近年来,杂环含硫Schiff碱及其金属配合物因其良好的抑菌、抗肿瘤活性引起了人们的广泛关注。以往的研究主要集中在吡啶类、呋喃类含硫Schiff碱及其过渡金属配合物上。而吡嗪类、噻唑类含硫Schiff碱及其过渡金属配合物则鲜有报道。本文的主要内容如下:1. 2-乙酰基吡嗪缩肼基二硫代甲酸苄酯Schiff碱及其金属配合物的合成与表征。合成了2-乙酰基吡嗪缩肼基二硫代甲酸苄酯Schiff碱及其双螫合锌(Ⅱ)、锰(Ⅱ)和单螯合的铜(Ⅱ)的金属配合物,并通过元素分析、质谱、红外光谱、电子光谱、核磁共振氢谱和摩尔电导等测试手段进行了表征,确定了其组成和可能的结构。2. 2-乙酰基噻唑缩肼基二硫代甲酸苄酯Schiff碱和2-乙酰基噻唑缩氨基硫脲schiff碱(?)合成了2-乙酰基吡嗪缩肼基二硫代甲酸苄酯Schiff碱和2-乙酰基噻唑缩氨基硫脲。并通过元素分析、质谱、红外光潜、核磁共振氢谱和核磁共振碳谱等测试手段进行了表征,确定了其组成和可能的结构。3. 2-乙酰基吡嗪缩肼基二硫代甲酸苄酯Schiff碱及其过渡金属配合物的抑菌活性研究。分别对2-乙酰基吡嗪缩肼基二硫代甲酸苄酯Schiff碱及其双螯合锌(Ⅱ)、锰(Ⅱ)和单螯合的铜(Ⅱ)的金属配合物测试了抑菌活性,实验菌株为革兰氏阳性菌(金黄色葡萄球菌、苏云金芽孢杆菌、巨大芽孢杆菌和枯草芽孢杆菌)和革兰氏阴性菌(大肠杆菌、铜绿假单孢菌和恶臭假单孢菌)。抑菌活性测试表明:(1) 配体和配合物对革兰氏阳性菌和革兰氏阴性菌均有一定的活性。(2) 配合物的活性强于配体的。(3) 化合物的活性和化合物的浓度不呈简单的线性关系,而是在一定浓度范围内有一个最大活性值。4. 对已合成化合物的抗稻瘟霉活性筛选为在已合成化合物中寻找抗肿瘤先导化合物,我们采用了稻瘟霉模型筛选法。抗稻瘟霉活性实验表明:上述化合物有不同程度的活性,而2-乙酰基噻唑缩肼基二硫代甲酸苄酯Schiff碱的活性最强。更多还原

【Abstract】 The wide variety of biological activity was exhibited by heterocyclic thiosemicarbazaones .In the recent research, more attention was paid to the Schiff bases and their metal complexes for their significant antibacterial and antitumor activity. Previous studies have centred mainly on transition metal complexes of sulfur-containing Schiff bases with pyridine or furan series. However the complexes of sulfur-containing Schiff bases with pyrazine or thiazole series were seldom reported. Our main job was described as below;l.Synthesis and Characterization of New Transition Metal Complexes with Schiff base ligands derived from S-benzyldithiocarbazate and 2-acetylpyrazine.New bis-chelated Zinc(II), Manganese(II) and mono- chelated Copper(II) complexes with Schiff base ligands derived from S-benzyldithiocarbazate and 2-acetylpyrazine were prepared. The compounds were characterized by elementary analysis, Mass spectrum,IR Spectra, Electronic Spectra, 1H NMR Spectra and Molar conductance measurements.And their composition and probably structure are confirmed.2. Synthesis and Characterization of New Schiff base ligands derived from S-benzyldithiocarbazate, thiosemicarbazone and 2-acetylthiazole.Two kinds of Schiff bases derived from S-benzyldithiocarbazate, thiosemicarbazone and 2-acetylthiazole were prepared. The compounds were characterized by elementary analysis, IR Spectra, Mass spectrum, 1H NMR, 13C NMR Spectra and their composition and probably structure are confirmed.3. The antibacterial activity of New Transition Metal Complexes with Schiff base ligands derived from S-benzyldithiocarbazate and 2-acetylpyrazine.The antibacterial activity of Schiff base ligands derived from S-benzyldithiocarbazate and 2-acetylpyrazine and their bis-chelated Zinc(II) , Manganese(II) and mon- chelated Copper(II) complexes have been tested against gram-positive bacterium (Staphylococcus aureus, Bacillus thuringiensis, Bacillus megateriumand Bacillus subitilis) and gram-negative bacterium(Escherichia coli, Pseudomomas aeruginosa and Pseudomomas putida). The antibacterial activity results are as follows:(1) the ligands and complexes are differently effective against gram-positive bacterium and gram-negative bacterium.(2) The antibacterial activity of the complexes is stronger than the ligands.(3) The antibacterial activity isn’t stronger when the concentration of the compound becames larger,but have the best effect in a certain range. 4. Screening of anti-pyricularia oryzae activity of the complexes that had been prepared.To seek forerunner antitumor drugs from compounds that had been prepared, the screening model of pyricularia oryzae was applied.The anti- pyricularia oryzae activity results showed that the compounds are differently effective against pyricularia oryzae ,and that activity of Schiff bases derived from S-benzyldithiocarbazate and 2-acetylthiazolc are strongest.更多还原