两种含二茂铁基schiff 碱的合成及其抑菌活性

通过乙酰基二茂铁与两种杂环胺(4-氨基安替比林,2-氨基-5-巯基-1,3,4-噻二唑)缩合合成了两种含二茂铁基的Schiff碱(a、b),产率分别为85.8%和72.6%,并通过IR、1HNMR及元素分析对其结构进行了确证。最后,将合成出的两种Schiff碱分别对3种细菌(金黄色葡萄球菌、大肠杆菌、枯草芽孢杆菌)进行了初步抑菌实验,将其结果与非杂环类Schiff碱Fc-C(CH3)NC6H5=(c)的抑菌性能做了比较。结果表明,Schiff碱对上述3种细菌都有抑制作用,且抑菌效果随着Schiff碱浓度的增大而增强。此外,杂环类Schiff碱(a、b)对上述3种细菌的抑菌活性明显优于非杂环类Schiff碱(c)。     

含噻吩双水杨醛席夫碱化合物的合成与抑菌活性

以5,5'-亚甲基双水杨醛和2-(2-氨基苯胺基)-3-氰基-5-甲基噻吩为原料合成了一种新颖的含噻吩双水杨醛Schiff碱化合物5,5'-亚甲基双水杨醛缩-2-(2-氨基苯胺基)-3-氰基-5-甲基噻吩席夫碱,而5,5'-亚甲基双水杨醛由水杨醛和三聚甲醛缩合制得。元素分析和质谱结果证实,该Schiff碱的分子式为C39H30N6O2S2,红外光谱和1HNMR确证了其结构。用牛津杯琼脂扩散法测定了标题化合物的抑菌性能,结果表明,该Schiff碱对4种菌均有一定的抑制效果,质量浓度为1.5 g/L时,对大肠杆菌的抑菌环直径达15.0 mm,其抑菌活性为大肠杆菌>枯草芽孢杆菌>金黄色葡萄球菌>表皮葡萄球菌。     

呋喃胺水杨醛Schiff碱镍(Ⅱ)配合物的合成与结构表征

以4,5-二甲基-3-腈基-2-呋喃胺与水杨醛为原料,合成了4,5-二甲基-3-腈基-2-呋喃胺水杨醛Schiff碱化合物,再与氯化镍反应得到一种新型的呋喃胺水杨醛Schiff碱镍(Ⅱ)配合物.通过IR、UV、元素分析及摩尔电导率等对目标化合物进行了表征,应用荧光光谱法研究了该配合物与牛血清白蛋白(BSA)在不同温度下...     

含硫双Schiff碱及其金属配合物的合成、表征与生物活性研究

合成了茚三酮-1,3-双缩肼基二硫代甲酸苄酯(HL1),茚三酮-1,3-双缩氨基硫脲(HL2)两种含硫双Schiff碱及它们的铜、钴金属等配合物,通过元素分析、红外光谱、紫外-可见光谱、差热和摩尔电导等测试对其进行了表征,并测试了双Schiff碱配体与金属配合物对大肠杆菌、枯草芽孢杆菌的抑菌活性。     

新型羟氨类HDAC抑制剂的合成

对羟氨类HDAC抑制剂化学合成方法进行探索研究,并在此基础上合成出新的系列衍生物。以苯胺、辛二酸单甲酯为原料合成N-苯-8-甲酯辛酰氨,在无水的条件下使甲酯变成羟氨,进而合成目标化合物suberoylanilide hydroxamic acid(SAHA);以反式4-氯-3-硝基肉桂酸,二乙氨基乙硫醇盐酸盐为原料,形成西佛碱,还原胺化,合成目标化合物反式-甲基-3-(4-(2-(二乙氨基)乙硫醇基)3-噻吩甲氨基)丙烯酸酯。在文献的基础上改进合成路线,合成出SAHA和新的SB939类衍生物反式-甲基-3-(4-(2-(二乙氨基)乙硫醇基)-3-噻吩甲氨基)丙烯酸酯,为进一步开展新药物研究和实际开发具有自主知识产权的药物打下基础。     

新型含芴Schiff碱化合物的合成及其紫外-可见光谱性能研究

通过9-芴甲醛与相应的芳胺衍生物反应合成了两种新型含芴Schiff碱化合物:9-亚甲基19-亚(2-氨基芴)基芴和9-亚甲基-9-亚(2-甲基苯胺)基芴,其结构经核磁共振谱、红外光谱和质谱表征.吸收光谱法测定了两种含芴Schiff碱衍生物在乙醇、四氢呋喃、环己烷和氯仿中的最大吸收波长(λmax),并探讨了分子结构和溶剂...     

芳香醛(酮)缩氨基硫脲的微波合成及其抗菌活性的研究

肼基二硫代甲酸甲酯与相应的醛或酮在微波辐射下经2~3.5 min反应,得到3-二取代甲(乙)撑肼基二硫代甲酸甲酯,产率91%~96%。再与胺在微波辐射下经35~45 min反应,得到目标化合物,产率80%~90%。合成的6个目标化合物通过熔点测定和质谱、红外光谱、核磁共振氢谱分析,对其结构进行确证,并测试了化合物的抑菌活性。     

4-氨基安替比林Schiff碱的合成及其抗O2-活性

合成了未见报道乙二醛双缩4-氨基安替比林、丁二酮双缩4-氨基安替比林和其它Schiff碱.对这些化合物进行了元素分析、红外、紫外和核磁谱的表征.对化合物进行了抗超氧阴离子活性的研究.试验表明,这些化合物都有抗超氧阴离子活性.     

糠醛双Schiff碱及其铜配合物的合成与抗菌活性研究

合成了糠醛双Schiff碱N,N′-双(2-呋喃甲醛亚胺基乙基)-2,6-吡啶二甲酰胺及其铜配合物,通过波谱分析对其结构进行了表征,测定了Schiff碱及其铜配合物对大肠杆菌、金黄色葡萄球菌和枯草芽孢杆菌的抗菌活性和最低抑菌浓度。结果表明,Schiff碱及其铜配合物均有一定的抗菌活性,且Schiff碱铜配合物的抗菌活性更好,两者最低抑菌浓度均在0.5~1.0 g.L-1之间。     

脱氢枞基含氮衍生物的抑菌活性研究

采用平板计数法研究了脱氢枞酸（1）和脱氢枞基含氮衍生物（脱氢枞胺（2）、脱氢枞酸酰胺衍生物（3a~3m）、脱氢枞胺（取代）苯甲醛Schiff碱衍生物（4a~4i））对6种病原真菌的抑制活性。结果表明：脱氢枞胺的抑菌活性优于脱氢枞酸,脱氢枞胺（取代）苯甲醛Schiff碱衍生物的抑菌活性优于脱氢枞酸酰胺衍生物。其中含卤原子的脱氢枞胺（对氯）水杨醛Schiff碱（4d）、脱氢枞胺（间氟）苯甲醛Schiff碱（4f）、脱氢枞胺（对氟）苯甲醛Schiff碱（4g）、脱氢枞胺（对氯）苯甲醛Schiff碱（4h）具有较强的抑菌活性,4h在质量浓度为180 mg/L时对灰葡萄孢、腐皮镰孢和芸苔链格孢的抑制率达100%,抑制率接近阳性对照物放线菌酮。进一步测定了脱氢枞胺（取代）苯甲醛Schiff碱衍生物4d、4f、4g和4h在不同质量浓度下对6种病原真菌的抑菌活性。结果发现4种化合物在不同质量浓度下对灰葡萄孢和芸苔链格孢均具有较好的抑制活性。化合物4f在22.5 mg/L时对6种病原真菌的抑制率最高,均大于95%,而4g在22.5 mg/L时的抑制率却最低,并且4h在45 mg/L时的抑制率较高,上述结果表明苯环上卤原子的取代位置和类型均会影响其在不同质量浓度下的抑菌活性和最佳抑菌活性的质量浓度。     

松香含氮衍生物对小地老虎四龄幼虫的拒食活性及构效关系

采用叶碟浸叶法,研究了4种不同类型的松香含氮衍生物对小地老虎4龄幼虫的拒食活性。结果显示：脱氢枞胺对氯水杨醛Schiff碱（2i）和二氢枞酸异丙醇酰基硫脲（4b）较大地抑制了小地老虎4龄幼虫的取食,质量浓度1 g/L时2i和4b 24 h后的拒食率分别为86.12%和85.13%;脱氢枞胺对甲氧基苯甲醛Schiff碱（2b）、二氢枞酸2-羟甲基-1,3-丙二醇酰基硫脲（4c）和二氢枞酸呋喃酰基硫脲（4g）对小地老虎4龄幼虫具有较强的拒食活性,拒食率分别为52.04%、66.70%和50.48%。2i具有极低的拒食中质量浓度（AFC₅₀）,为0.04 g/L,2b、4b、4c和4g的AFC₅₀分别为0.66、0.25、1.47和0.69 g/L。脱氢枞胺（取代）苯甲醛Schiff碱和二氢枞酸酰基硫脲2类衍生物对小地老虎具有较强的拒食活性,甲氧基、氯原子和羟基对脱氢枞胺（取代）苯甲醛Schiff碱的拒食活性有明显的增强作用,二氢枞酸酰基硫脲衍生物中羟基的位置和个数对小地老虎4龄幼虫的拒食活性有明显的影响。脱氢枞酸酰胺和脱氢枞酸酰基硫脲衍生物对小地老虎4龄幼虫的拒食活性较弱,且其结构变化对小地老虎4龄幼虫的拒食活性影响较小。     

3-对盖烯-1-胺及其席夫碱衍生物的抑菌活性研究

利用微量肉汤稀释法测定3-对烯-1-胺（1）及其席夫碱衍生物（2a~2l）对革兰氏阳性菌金黄色葡萄球菌、革兰氏阴性菌肺炎克雷伯氏菌及真菌白色念珠菌的抑菌活性,并讨论了构效关系。结果表明：3-对烯-1-胺及其部分席夫碱衍生物对这3种菌具有一定的抑菌活性,其中化合物1对金黄色葡萄球菌的抑菌活性最强,最小抑菌浓度（MIC）值为56.25 mg/L;化合物2h和2i对肺炎克雷伯氏菌的抑菌活性最强,MIC值均为112.5 mg/L;化合物2l对白色念珠菌的抑菌活性最强,MIC值为28.125 mg/L。构效关系分析结果表明：向3-对烯-1-胺席夫碱衍生物中引入Br、Cl等卤素后,能显著增强抑菌活性;含有吡啶环的3-对烯-1-胺席夫碱衍生物对真菌白色念珠菌的抑菌活性明显要高于含呋喃环、吡咯环或噻吩环的3-对烯-1-胺席夫碱衍生物。     

Preparation and antibacterial activity of C2-benzaldehyde-C6-aniline double Schiff base derivatives of chitosan

C₂-benzaldehyde-C₆-aniline double Schiff base derivatives of chitosan were synthesized with positioning protection method for the first time. The structures and properties of the new synthesized products were characterized by Fourier transform infrared spectroscopy, ¹³C nuclear magnetic resonance, scanning electron microscope image, X-ray diffraction, and elemental analysis. The elemental analysis results indicated that the degrees of substitution of the products were from 39.6% to 48.2%. The synthesized compounds exhibited an excellent solubility in organic solvents. The antibacterial activities of all of the derivatives were tested in the experiment, and the results showed that the prepared chitosan derivatives had significantly improved antibacterial activity of chitosan and C₂-benzaldehyde Schiff bases of chitosan toward Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 35218). Antibacterial activity of the Schiff bases against E. coli differs from the substituent at the same position of different anilines and increases as the sequence aniline?>?p-toluidine?>?o-toluidine, and the antibacterial activity of the Schiff bases against S. aureus increases as the sequence p-toluidine?>?aniline?>?o-toluidine. The I_C50 of the C₂-benzaldehyde-C₆-aniline double Schiff base derivatives of chitosan against E. coli and S. aureus is 0.0035 and 0.0031?mg?L^?1, respectively, much lower than that of chitosan (0.0064?mg?L^?1) and C₂-benzaldehyde Schiff bases of chitosan (0.0054?mg?L^?1). The cytotoxicity test showed that compared with chitosan and C₂-benzaldehyde Schiff bases of chitosan, the prepared chitosan derivatives had lower cytotoxicity against SCG-7901. This paper provided a new method for the synthesis of Schiff bases of chitosan, which was enlightening.     

Synthesis of polymer-supported metal-ion complexes and evaluation of their catalytic activities

Polymer-supported transition-metal-ion complexes of the N,N′-bis(o-hydroxy acetophenone) propylenediamine (HPPn) Schiff base were prepared by the complexation of iron(III), cobalt(II), and nickel(II) ions on a polymer-anchored N,N′-bis(5-amino-o-hydroxy acetophenone) propylenediamine Schiff base. The complexation of iron(III), cobalt(II), and nickel(II) ions on the polymer-anchored HPPn Schiff base was 83.44, 82.92, and 89.58 wt%, respectively, whereas the unsupported HPPn Schiff base showed 82.29, 81.18, and 87.29 wt % complexation of these metal ions. The iron(III) ion complexes of the HPPn Schiff base showed octahedral geometry, whereas the cobalt(II) and nickel(II) ion complexes were square planar in shape, as suggested by spectral and magnetic measurements. The thermal stability of the HPPn Schiff base increased with the complexation of metal ions, as evidenced by thermogravimetric analysis. The HPPn Schiff base showed a weight loss of 51.0 wt % at 500°C, but its iron(III), cobalt(II), and nickel(II) ion complexes showed weight losses of 27.0, 35.0, and 44.7 wt % at the same temperature. The catalytic activity of the unsupported and supported metal-ion complexes was analyzed by the study of the oxidation of phenol and epoxidation of cyclohexene in the presence of hydrogen peroxide. The supported HPPn Schiff base complexes of iron(III) ions showed a 73.0 wt % maximum conversion of phenol and 90.6 wt % epoxidation of cyclohexene, but unsupported complexes of iron(III) ions showed 63.8 wt % conversion of phenol and 83.2 wt % epoxidation of cyclohexene. The product selectivity for catechol (CTL) and epoxy cyclohexane (ECH) was 93.1 wt % and 98.1 wt % with the supported HPPn Schiff base complexes of iron(III) ions, but it was low with the supported Schiff base complexes of cobalt(II) and nickel(II) ions. The selectivity for CTL and ECH varied with the molar ratio of the metal ions but remained unaffected by the molar ratio of hydrogen peroxide to the substrate. The energy of activation for the epoxidation of cyclohexene and oxidation of phenol with the polymer-supported Schiff base complexes of iron(III) ions was 10.0 and 12.7 kJ/mol, respectively, but it was found to be higher with the supported HPPn Schiff base complexes of cobalt(II) and nickel(II) ions and with the unsupported HPPn Schiff base complexes of iron(III), cobalt(II), and nickel(II) ions. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci 2008     

乙二胺水杨醛双Schiff碱Cr（Ⅲ）配合物的合成与表征

以水杨醛与乙二胺为原料合成乙二胺水杨醛双Schiff碱,并进一步与Cr（Ⅲ）络合得到金属配合物;采用元素分析、紫外可见吸收光谱、红外光谱对乙二胺水杨醛双Schiff碱及其Cr（Ⅲ）配合物的结构进行了表征。结果表明,合成的乙二胺水杨醛双Schiff碱配体及其Cr（Ⅲ）配合物的分子结构与理论结构相符;乙二胺水杨醛双Schiff碱配体及其Cr（Ⅲ）配合物均有一定的抗菌活性,且Cr（Ⅲ）配合物的抗菌活性更好。     

邻苯二甲醛双缩氨基硫脲Schiff碱及其银配合物的合成与表征

Schiff碱及其配合物具有特殊的结构和性质。文章以邻苯二甲醛（OPA）和氨基硫脲为原料,在不同反应条件下合成出一种对称的邻苯二甲醛双缩氨基硫脲Schiff碱配体,并制备出其银配合物。通过红外光谱、紫外光谱、元素分析等手段对配体及配合物的结构进行了初步表征。测定了银配合物的电导性能。抑菌试验结果表明,配体和银配合物对金黄色葡萄球菌、枯草芽孢杆菌、大肠杆菌均有不同程度的抑菌效果。     

Corrosion inhibition and Biocidal effect of some cationic surfactants based on Schiff base

The three cationic surfactants based on Schiff base were laboratory prepared, (E)-decyl-4-[(2-hydroxyethylamino) methyl]-N,N-dimethyl benzenaminium bromide (I), (E)-dodecyl-4-[(2-hydroxyethylamino)methyl]-N,N-dimethyl benzenaminium bromide (II) and (E)-hexadecyl-4-[(2-hydroxyethylamino)methyl]-N,N-dimethyl benzenaminium bromide (III) were evaluated as corrosion inhibitors for carbon steel in acid medium and antimicrobial agents against sulfate reducing bacteria, SRB. Three techniques were used for the corrosion inhibition evaluation, namely; weight loss, polarization and electrochemical impedance. The serial dilution method was used to evaluate the inhibiting effect of these compounds on the sulfate reducing bacteria growth. The results showed that the prepared compounds have good antimicrobial activities against the SRB as well as they have high efficiency as corrosion inhibitors for carbon steel in 1 M HCl.     

水杨醛双Schiff碱与其铜配合物的合成与抗菌活性研究

文章首先合成了水杨醛双SchiffN,N’-双（2-水杨醛亚胺基乙基）-2,6-吡啶二甲酰胺（Iia）,并以它为配体合成了铜配合物,通过波谱分析对其结构进行了表征。并采用固体培养基抑菌圈法和液体培养基比浊法对了Schiff碱及其铜配合物进行抗菌活性的测定。结果表明,水杨醛双Schiff碱及其铜配合物对大肠杆菌和金黄色葡萄球菌均有抗菌活性,并且水杨醛双Schiff碱铜配合物的抗菌活性比水杨醛双Schiff碱的抗菌活性强。     

Synthesis,Biological Study and Complexation Behavior of Some Anionic Schiff Base Amphiphiles

A novel series of anionic Schiff base amphiphiles were synthesized. The chemical structures of these compounds were elucidated using different spectroscopic tools. The surface and thermodynamic properties of the prepared Schiff bases were studied using classical measurements including surface and interfacial tensions. The surface parameters of these compounds, e.g., surface tension, critical micelle concentration, effectiveness, efficiency, maximum surface excess, minimum surface area, and interfacial activity showed their good surface activity. Their thermodynamic parameters of adsorption and micellization including free energy change of micellization and adsorption showed their tendency toward adsorption at the interfaces and also micelle formation at lower concentrations. The complexation behavior of the synthesized Schiff bases were study through the interaction of the Schiff base (IIIa; SBSD) with nickel chloride hexahydrate. All synthesized compounds in addition to NiCl₂·6H₂O and Ni Schiff Base complex have been evaluated for their antibacterial activity against Gram-positive and Gram-negative bacteria. The results of the biocidal activities showed high potent action of (Ni-III_a; Ni-SBSD) complex more than Schiff base IIIa; SBSD.