对氟苯胺Schiff碱的合成及其生物活性研究

本文报道用5－硝基水杨醛合成了5－硝基,N（对氟苯基）水杨醛亚胺Schiff碱,其结构用红外光谱和共振谱表征,并对其生物活性作了初步研究,发现该化合物具有比较好的抑菌能力。     

多基硫脲类Schiff碱的合成及生物活性与离子识别

以异硫氰酸苯酯、氨基硫脲、乙二胺、氨基脲和二乙撑三胺为原料,合成了异硫氰酸苯酯-氨基甲酰肼(PITCAM)、异硫氰酸苯酯-硫代氨基脲(PITCTSC),双异硫氰酸苯酯-1,2-二氨基乙烷(PITCE)和双异硫氰酸苯酯-二乙撑三胺(PITCD)4种多基硫脲类Schiff碱,其结构经1HNMR、IR、ESI-MS和元素分析进行表征.对4种合成的化合物进行抑制大肠杆菌、金黄色葡萄球菌以及欧文氏草生杆菌的生物活性测定,结果表明4种合成的多基硫脲类Schiff碱化合物均具有一定的生物抑菌活性,其中合成的化合物PITCAM的生物抑菌活性最好;测试其对不同金属离子的荧光响应光谱,实验结果表明PITCAM对Cu2响应明显.     

含Schiff碱结构的2-芳胺基嘧啶衍生物的合成及体外抗肿瘤活性研究

以邻甲基苯胺、3-乙酰基吡啶、N,N二甲基甲酰胺二甲基缩醛为起始原料,经硝化、加成、环合、还原、缩合等6步反应合成目标化合物。以伊马替尼为阳性对照药,采用台盼蓝排染法,以慢性粒细胞白血病K562细胞为测试细胞株,对目标化合物进行体外抗白血病活性评价。所合成的18个化合物结构经1HNMR和MS确证。初步药理实验结果表明,目标化合物对K562细胞有一定的抗肿瘤活性,但低于阳性对照药伊马替尼和先导化合物。酰胺键结构对保持活性有重要的影响,是药物与受体的重要结合位点。     

希夫碱配合物生物活性方面的应用研究进展

综述了希夫碱类化合物在抑菌、杀菌、抗肿瘤、抗病毒等方面的生物活性,并且对其生物活性在医药上的应用做出了展望.     

香兰素邻甲苯胺席夫碱及其铜(Ⅱ)配合物的合成与抑菌性探究

合成香兰素缩邻甲苯胺及其铜配合物,对合成的物质进行了表征,并采用滤纸片扩散法测定配体和配合物对黑曲霉、木霉、立枯丝核菌、尖镰孢菌黄瓜专化型四种菌种的抑菌作用,实验结果表明:配体和配合物对这四种菌的生长都有一定的抑制作用,其中配体和配合物对黑曲霉具有较强的抑制作用。     

吡唑席夫碱化合物的合成及其生物活性研究

以乙酰丙酮、水合肼、取代苯甲醛为起始原料,经过肟化、缩合反应得到一系列新型吡唑席夫碱化合物,通过元素分析、。HNMR、FTIR、MS等对目标化合物结构进行表征,并采用平皿法测试了目标化合物对单子叶植物玉米的生长调节活性。结果表明,目标化合物在低浓度下对玉米的生长表现出促进作用,尤以10mg·L-1浓度下对玉米生长的促进作用最显著,高浓度下对玉米的生长表现出显著抑制作用。     

酰基吡唑啉酮希夫碱及配合物的合成、结构及生物活性

综述了酰基吡唑啉酮希夫碱及配合物的合成、结构和生物活性.介绍了非水溶剂法、固相合成法、水相合成法、溶剂热合成法等配合物合成方法.分析了酰基吡唑啉酮希夫碱参与过渡金属、稀土金属配位成键的方式,以及相应配合物空间构型为四面体、平面正方形、八面体、十二面体的结构关系.讨论了标题化合物对金黄葡萄球菌、枯草杆菌、大肠杆菌等的抑制...     

Synthesis, Characterization and Biological Activity of Sugar-Based Gemini Cationic Amphiphiles

Two series of gemini cationic surfactants were synthesized based on glucose and fructose molecules. Their chemical structures were confirmed using micro-elemental analysis, mass spectral fragmentation and FTIR spectroscopic analysis. The surface activities of these gemini amphiphiles were measured, including surface tension (γ), critical micelle concentration (CMC), effectiveness (π _cmc), efficiency (pC₂₀), maximum surface excess (Γ_max) and minimum surface area (A _min) at 25 °C. Adsorption and micellization free energies of these amphiphiles in their solutions showed a good tendency towards adsorption at the interfaces. The biological activity of the synthesized gemini amphiphiles showed good inhibition at concentrations of 1, 2.5 and 5 mg/mL. The synthesized amphiphiles showed antimicrobial activity on gram-positive and gram-negative bacteria and antifungal activity equal to or comparable to commercially available controls. The discussion rationalized the antimicrobial activities of these amphiphiles with the surface activity and the adsorption parameters. In addition, the effect of sugar nuclei was discussed based on the chemical structure of the bacterial and fungal cell membranes.

壳聚糖缩糠醛Schiff碱合成研究

文章由壳聚糖与糠醛缩合反应合成了一种Schiff碱,通过L934正交实验法,对合成的反应温度、反应时间、pH和反应物的配比进行了优化。得到了制备的最佳条件:pH=9,反应物配比n(壳聚糖结构单元):n(糠醛)=1:4,反应温度70℃,反应时间3h。此时,壳聚糖缩糠醛Schiff碱的缩合产率最大为85.47%。合成的Schiff碱是一种双烯体,可用于双烯合成反应。并通过FTIR、UV对Schiff碱的结构进行了表征。     

含三唑Schiff碱硫醚衍生物的合成及生物活性研究

以2,4-二氯苯甲酸为起始原料,经酯化、肼解、成盐、闭环合成3-硫酮-4-氨基-5-(2,4-二氯)苯基-1,2,4-三唑(Ⅳ),然后与取代甲醛缩合生成中间体(Ⅴ),最后以乙腈为溶剂,K2CO3为催化剂,中间体Ⅴ与卤代烃于75℃反应2 h合成了8个含三唑Schiff碱硫醚衍生物(Ⅵa~Ⅵh),收率69%~78%,其结构经1HNMR、13CNMR、19FNMR、IR以及元素分析表征。初步生物活性测试结果表明,部分目标化合物对黄瓜霜霉病的抑制率达100%。     

Synthesis and Evaluation of Surface and Biological Properties of Some Lactic Acid-Based Anionic Surfactants

In the present study, 11 lactic acid-based anionic surfactants were synthesized and evaluated for their surface and biological activities. The synthesis involved the esterification of lactic acid with a range of fatty alcohols differing in chain length as well as in branching and unsaturation. The resultant ester was sulfonated by treatment with chlorosulfonic acid followed by salt formation with aqueous NaOH solution. The surface properties of all the synthesized surfactants were determined using surface tensiometry. Synthesized surfactants showed low critical micelle concentration (CMC) values and a decreasing trend with an increase in the alkyl chain length. Alkyl branching also led to a mild change in CMC values when compared with linear counterparts having the same number of carbon atoms, though such decreases or increases were observed to be dependent on the position and number of the branching. Some of the synthesized surfactants exhibited good antimicrobial and anti-cancer activities against the tested microbial strains and cell lines.     

Synthesis,Surface Activity and Aggregation Behavior of Novel Gemini Pyridinium Amphiphiles

A series of novel pyridinium cationic gemini amphiphiles, 3,3′-(carbonyldiimino)bis (1-n-alkylpyridinium) dibromides, having octyl, decyl, dodecyl, tetradecyl alkyl chains were synthesized. The surface properties and aggregation behavior in aqueous solution were evaluated by surface tension, dynamic light scattering (DLS), and transmission electron microscopy (TEM) measurement. The adsorption at the air/solution interface of all the compounds were quantitative described using the Frumkin model, and the effect of alkyl chain length on surface activity and aggregate behavior was analyzed. It was found that all the gemini amphiphiles possess surface activity and low critical micellization concentration (CMC) values. The values of log CMC depended linearly on the carbon number of the alkyl chains, but the surface tension at the CMC (γ_cmc) showed a minimum for the compound with dodecyl chains. Combinations of DLS and TEM observations showed the existence of vesicles with a broad size distribution in aqueous solution. Meanwhile, vesicles formed below the CMC could be a possible reason for the observed deviation of surface tension curves from the Frumkin model.     

新型席夫碱缓蚀剂的合成及性能研究

以苯甲醛、A胺为原料合成一种席夫碱酸化缓蚀剂,通过正交试验优化得出最佳合成条件如下:n(胺):n(醛)=0.8,反应时间8h,反应温度60℃,催化剂加量为0.5%。用失重法评价了席夫碱在盐酸溶液中的缓蚀性能。在15%盐酸中,当缓蚀剂加量为1.0%时,N80钢片的腐蚀速率为0.9534 g·(m2·h)-1,低于SY/T 5405-1996《酸化用缓蚀剂性能试验方法及评价指标》中的一级标准。     

一种新希夫碱的合成

由对羟基苯乙酮与氯乙酸甲酯反应,得到一种酮,这种酮再与乙醇胺反应得到一种新的希夫碱。根据这种新希夫碱结构特点,对它的应用前景作了展望。     

N-氨基喹啉席夫碱盐的合成

以硫酸羟胺和氯磺酸为原料,合成了N-氨基喹啉碘化物。在乙醇溶剂中N-氨基喹啉碘化物与间硝基苯甲醛反应,形成了新的N-氨基喹啉席夫碱盐。采用元素分析,FT-IR,1HNMR对目标化合物进行了结构分析。     

过渡金属组氨酸水杨醛Schiff碱配合物的合成及生物活性

合成了四种组氨酸水杨醛$chiff碱过渡金属配合物[Cu(His-Sal)、Ni(His-sal)、Co(His-Sal)、Mn(His-Sal),His=组氨酸,Sal=水杨醛],其结构经UV、IR,元素分析,摩尔电导分析表征.荧光光谱表明四种配合物都能强烈猝灭BSA的内源荧光.生物活性实验表明配合物对金黄色葡萄球菌...     

水溶性席夫碱型大环化合物的合成方法研究

报道以磺基水杨醛、1,3-二氯-2-丙醇为原料,采用超声波催化法合成中间体1,3-双(2'-甲酰-4'-磺酸钠)苯基-1,3二氧-2-丙醇(2),然后中间体(2)再与邻苯二胺反应得到了水溶性席夫碱型大环化合物(3).并对合成中间体1,3-双(2'-甲酰-4'-磺酸钠)苯基-1,3二氧-2-丙醇的超声波催化法与常规加热法...     

Some Schiff Base Surfactants as Steel-Corrosion Inhibitors

Two series of Schiff base amphiphiles were prepared by condensation of benzaldehyde or anisaldehyde with three different alkyl chain length fatty amines namely: dodecyl, hexadecyl and octadecyl amine. The chemical structures of the prepared Schiff bases were confirmed by using different techniques, (elemental analysis, FTIR and ¹H-NMR spectra). The data of structural analysis for these compounds were confirmed by the purity of the synthesized amphiphiles. The synthesized Schiff bases were evaluated as corrosion inhibitors for low carbon steel (mild steel) in various acidic media (HCl and H₂SO₄) using a weight loss technique. The corrosion inhibition measurements of these inhibitors showed high protection against corrosion process in the tested acidic media at different doses (50, 100, 150 and 200 ppm) as well as their having a good biocidal effect against sulphate reducing bacteria. The discussion correlated the efficient corrosion inhibition of these inhibitors to their chemical structures.     

席夫碱锌酞菁的合成及性能

以4-硝基邻苯二甲腈为主要原料,合成两种席夫碱锌酞菁:2(3),9(10),16(17),23(24)-四(4-苯亚胺苯氧基)锌酞菁(C84H52N12O4Zn)(APc)和2(3)-[(2-甲基-8-羟基喹啉基]-9(10),16(17),23(24)-三(4-苯亚胺苯氧基)锌酞菁(C81H50N12O4Zn)(BPc)。通过核磁、红外、紫外、元素分析手段对其结构进行表征。结果表明,浓度在1.499×10-5~2.407×10-5mol/L时,APc有J聚集存在,而BPc在所测浓度范围内不发生聚集;APc和BPc的Q带的最大吸收峰分别在672 nm和676 nm,与无取代的酞菁锌669 nm相比,明显红移。采用循环伏安法对其电化学性质和能级结构进行研究,这两种锌酞菁的LUMO(-5.411 eV,-5.384 eV)和HOMO(-4.214 eV,-4.210 eV)与纳米TiO2导带能级匹配。     

空间不对称希夫碱(HCBP-PHEN-SALH)的合成和表征

报道了用控制反应物配比的方法,合成空间不对称希夫碱5-氯-2-羟基二苯甲酮缩邻苯二胶缩水杨醛（HCBP-PHEN-SALH）,用红外光谱和核磁共振进行了结构表征。