Synthesis, Spectral Properties, Antibacterial and Antitumor Activity of Salinomycin Complexes with the Transition Metal Ions Co（ll）, Ni（ll）, Cu（ll） and Zn（ll）

SalNa （sodium salinomycin） reacts with divalent transition metal ions of Co（II）, Ni（II）, Cu（II） and Zn（II） to produce novel compounds characterized by various spectroscopic methods. The interaction of metal （II） ions with SalNa results in the formation of mononuclear complexes of a general composition of [M（Sal）2·（H2O）2] nH2O （n = 0 or 2） where the divalent cations replace Na~ ions from the cavity of initial compound. The new compounds （disalinomycinates） possess an enhanced antibacterial activity against Gram-positive microorganisms as compared to both SalNa and SalH （salinomycinic acid）, respectively. The metal （II） complexes manifest strong concentration dependent cytotoxic effect in experiments using human leukemia cell lines. The complexes of Co0I） and Cu（lI） proved to exert superior activity as compared to the Ni（II） and Zn（II） analogues and are much more cytotoxic than SalNa and SalH. Further studies should be conducted to determine the therapeutic indexes of the new compounds.

Synthesis, Characterization, Antibacterial, and Antifungal Activities of Cobalt(II), Nickel(II) and Copper(II) Complexes with 3-thioacetyl-2-amino-1,4-naphthoquinone and 2-benzoyl-3-amino-1,4-naphthoquinone Ligands

The aim of this work is to synthesize, characterize and evaluate the biological activity of 1,4-naphthoquinone derivatives ligands and their metal—Co(II), Ni(II) and Cu(II) chelates. Continuing our work with another derivatives of 1,4-naphthoquinone ligands, this work had been constructed for synthesis of new ligands derived from 1,4-naphthoquinone such as 3-thioacetyl-2-amino-1,4-naphthoquinone and 2-benzoyl-3-amino-1,4-naphthoquinone (L1-L2) which characterized on the basis of elemental analysis, electronic, IR, mass, 1H-NMR spectral data. The synthesized ligands have been carried out to achieve the coordination behavior towards bi-valent metal ions like cobalt, nickel and copper. The solid chelates of the different ligands were prepared and subjected to analytical techniques such as elemental analyses, spectroscopic techniques including mass, 1H-NMR, and IR spectroscopy, and thermal analyses techniques. The chelates were found to have octahedral geometry. The biological activity of the prepared ligands and their binary metals complexes were also screened against different antifungal and antibacterial organisms.

Coordination Behavior and Biological Activity of Some Transition Metal Complexes with 2-Acetyl and 2-Formyl-3-Amino-1,4-Naphthoquinone Ligands

The aim of this work is to synthesize, characterize and evaluate the biological activity of 2-acetyl and 2-formyl-3-amino-1,4-naphthoquinone (L1 - L2) and their metal-Co(II), Ni(II) and Cu(II) chelates. The newly chelates were characterized by elemental analysis, IR, mass and 1HNMR spectra, thermogravimetric analysis (TGA) and biological activity. The antibacterial and antifungal activities of the ligands and its metal complexes were screened against bacterial species (Staphylococcus aureus, Bacillus subtilis and Escherichia coli) and fungi (Candida albicans). Ampicillin and amphotericin were used as references for antibacterial and antifungal studies. The activity data show that the metal complexes have a promising biological activity comparable with parent free ligand against bacterial and fungal species.

Biological Activities of Schiff Bases and Their Complexes: A Review of Recent Works

Schiff bases are the most widely used organic compounds. They have been shown to exhibit a broad range of biological activities, including antifungal, antibacterial, antimalarial, antiproliferative, anti-inflammatory, antiviral, and antipyretic properties. This review summarizes the synthesis and biological activities of Schiff bases and their complexes.

Metal Complexes of Antibiotic Pipemidic Acid

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Synthesis and Characterization of Schiff Base Metal Complexes Derived from Cefotaxime with 1<i>H</i>-indole-2,3-dione (Isatin) and 4-N,N-dimethyl-aminobenzaldehyde

This work involved the synthesis of two Schiff base derivatives of cefotaxime antibiotic (CFX) namely: [sodium3-(acetoxymethyl)-7-((Z)-2-(methoxyimino)-2-(2-((E)-2–oxoindolin-3-ylide-neamino) thiazol-4-yl)acetamido)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate]. (0.5) Methanol (LI) and [sodium3-(acetoxymethyl)-7-((2Z)-2-(2-(4-dimethylamino) benzylideneamino) thiazol-4-yl)-2-(methoxyimino)acetamido)-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2-ene-2-carboxylate]. (0.5) Methanol (LII) from the condensation reaction of the antibiotic with 1H-Indole-2,3-dione(isatin) and -N, N-dimethyl amino benzaldehyde respectively. Metal complexes of the two Schiff base ligands with Co(II), Ni(II), Cu(II), Cd(II), Pd(II) and Pt(IV) ions were prepared by reacting each ligand with the metal salts in refluxing ethanol. The chemical structures of the two ligands as well as the stereo-chemical structures and geometries of the studied metal complexes were suggested depending the results obtained from CHN and TG analysis, NMR, FTIR, and atomic absorption spectrophotometry, electronic spectra, magnetic moments and conductivity measurements. The mole ratio of the ligands to the metal ion was 1:1 with tridentate bonding behaviors of the coordinating ligands with the metal ions.

Preparation and antibacterial activities of metal complexes of norfloxacin

The metal complexes of norfloxacin were prepared, and their structures were characterized using spectroscopic techniques like IR, 1H NMR, UV, atomic absorption, and CHN analysis. The solubility, melting point, and conductance measurements were also performed. These studies suggested that norfloxacin formed complexes with the metals utilizing carbonyl oxygen atom of the ring and carboxylic group oxygen atom. The antibacterial activities of these metal complexes against 14 different Gram-positive and Gram-negative microorganisms were studied by the disk susceptibility method. It was observed that the complexes of norfloxacin with magnesium, calcium, cobalt, nickel, and copper showed improved activity compared with the stated drug.

Syntheses, Supramolecular Structures and Antibacterial Activities of Five Helical Transition Complexes with 5-Chloro-1-phenyl-1 H-pyrazole-3,4-dicarboxylic Acid

Five new transition metal complexes [Cu（HL）2（H20）2] （1）, [Cu（HL）z（phen）] （2）, [Cu（HL）2（H20）]2（4,4′-bipy） （3）, [Zn（HL）2（HzO）2].（4,4′-bipy） （4）, [Ag（HL）（4,4′-bipy）]n （5）, （H2L=5-chloro-l-phenyl-lH-pyrazole-3,4-dicarboxylic acid, phen=1,10-phenanthroline; 4,4′-bipy = 4,4′bipyridine） have been synthesized and characterized. Complexes 1, 2 and 4 exhibit monomeric structures, 3 shows a dinuclear structure, 5 displays 1D chain structure, and all extend to 3D supramolecular network via rich hydrogen bonds. Complexes 1, 2, 3, 5 comprise single helical chains, while complex 4 generates quadruple-stranded helical chains. Furthermore, the antibacterial activities of the titled complexes against bacterial species, three Gram positive bacteria （Staphylococcus aureus, Bacillus subtilis and Candida albicans） and two Gram negative bacteria （Escherichia coli and Pseudomonas aeruginosa） were stud-ied and compared to the activities of free ligands by using the microdilution method.

4取代三联吡啶锌金属配合物的抗菌活性研究

试验旨在研究4取代三联吡啶锌金属配合物的抗菌活性。采用微量肉汤稀释法测定4取代三联吡啶锌金属配合物对金黄色葡萄球菌、沙门氏菌、大肠杆菌、铜绿假单胞菌、副溶血弧菌和无乳链球菌的最小抑菌浓度(MIC),观察经配合物作用后的细菌生长情况、菌体细胞形态、细胞膜通透性及胞内蛋白表达量的变化,探究其对金黄色葡萄球菌的抗菌作用机制。结果显示,4取代三联吡啶锌金属配合物对金黄色葡萄球菌、副溶血弧菌具有较高的抗菌活性,经配合物作用后的金黄色葡萄球菌生长延迟、菌体发生干瘪破裂、细胞膜通透性增强及胞内蛋白表达量减少。研究表明,4取代三联吡啶锌金属配合物可能通过破坏菌体或抑制蛋白表达而抑制细菌活性。

Antimicrobial, anticancer and DNA binding studies of transition metal(Ⅱ)complexes containing 2-phenyl-4-selenazole carboxylic acid

Three novel transition metal complexes [ML2（phen）]＇H20 （M= Mn, Co, Zn; HL= C10H702NSe, 2-phenyl-4-selenazole carboxylic acid, phen= 1,10-phenanthroline） 1-3 were synthesized and characterized by elemental analysis, IR spectra. Their crystal structures were deterimined by single-crystal X-ray diffraction method. The antibacterial activities of the complexes against five species of bacteria, Escherichia coli （E. coli）, Staphylococcus epidermidis （S. epidermidis）, Staphylococcus aureus （S. au- reus）, Acinetobacter baumanii （A. baumanii） and Streptococcus viridans （S. viridans）, were tested respectively. The anticancer activities of the complexes against human pancreatic cancer line PANC-28 and human hepatocarcinoma line HuH7 were also studied. The interactions between the complexes and DNA were studied by ethidium bromide （EB） fluorescent probe.

金属类化合物在抗菌领域的应用现状及展望

金属有机络合物具有悠久的临床应用历史,在治疗高血压、皮肤感染和胃肠道疾病方面表现出显著效果。随着近年来研究的进展,金属类化合物在抗细菌感染治疗中的应用及其作用机制受到了广泛地研究。笔者以3种常用金属类化合物为例,综述了金属类化合物在抗菌领域的研究进展、作用机制,并阐述了新型含金属药物以及中药提取成分及其衍生物金属络合物的研究动态,分析了金属药物在抗菌领域的潜在优势。

N－亚水杨基氨基酸3d金属配合物的合成、表征和抑菌活性

合成了丙氨酸、亮氨酸水杨醛席夫碱及其与Ｍｎ（Ⅱ）、Ｃｏ（Ⅱ）、Ｎｉ（Ⅱ）、Ｚｎ（Ⅱ）、Ｃｕ（Ⅱ）的配合物。通过元素分析、摩尔电导、磁化率、红外光谱和电子光谱等进行了表征。用ｐＨ法测定了配合物稳定常数。实验发现，配合物抑菌活性优于配体抑菌活性。

二氨基硫脲双核席夫碱和其配合物的合成与抗菌活性

以3-羧基水杨醛与二氨基硫脲为原料合成了新的3-羧基水杨醛双缩二氨基硫脲席夫碱（H4L）及其Co（Ⅱ），Ni（Ⅱ），Cu（Ⅱ），Zn（Ⅱ）双核配合物，收率57％～78％。通过元素分析、^1H NMR、IR、UV—Vis、摩尔电导、质谱分析等测试技术对合成得到的席夫碱化合物的组成和结构进行表征。抗菌活性结果表明，合成的席夫碱化合物具有较好的抗菌活性。

脱氢枞胺(5-硝基)水杨醛Schiff碱及其金属配合物的合成、晶体结构及性质研究(英文)

合成了脱氢枞胺(5-硝基)水杨醛Schiff碱及其Cu2+、Zn2+、Co2+和Ni2+配合物,用IR、1HNMR,UV-vis,摩尔电导及单晶X射线衍射对其进行结构表征。Cu(L)2形成经典的N2O2配体配合物,属于单斜晶系,C2空间群,晶胞参数为:a=3.6996nm,b=1.0835nm,c=1.2856nm,α=90°,β=103.36°,γ=90°。研究了溶剂的极性对配体和配合物紫外光谱变化的影响,当改变溶剂时,配体能发生分子内质子转移,从醇式结构变成酮式结构。金属配合物能溶于有机溶剂,摩尔电导率数据表明它们在二甲基甲酰胺、氯仿和甲苯中是非电解质,容易发生溶致变色性能。对配体及配合物进行了抑制大肠杆菌、金黄色葡萄球菌及枯草芽苞杆菌的生物活性测定,配体及配合物都表现出一定的生物活性,其中Cu配合物的活性最强,说明配合物的生物活性与金属有关。

新型吡唑Schiff碱及金属配合物的合成和抑菌活性

以3-氨基-4-氰基吡唑和芳醛为原料合成了10个新型吡唑Schiff碱及铜(II)、镍(II)、锌(II)、钴(II)4个金属配合物.用元素分析,IR,1HNMR及单晶解析表征了Schiff碱及金属配合物的结构.测定了Schiff碱及金属配合物对金黄色葡萄球菌、大肠杆菌、枯草杆菌和绿脓杆菌的抑菌活性.生物活性研究表明,Schiff碱及金属配合物对金黄色葡萄球菌、大肠杆菌和绿脓杆菌都有较好的抑菌效果,其中铜(II)和锌(II)配合物对金黄色葡萄球菌和大肠杆菌的抑菌活性最好.

几种酰代吡唑啉酮金属配合物的合成、抑菌活性及与DNA的相互作用

以4-呋喃甲酰基PMP和4-吡啶甲酰基PMP希夫碱衍生物为母体,分别合成了七种含铜、镧和钆的金属配合物,通过红外、紫外吸收光谱、元素分析等对配体及配合物的结构进行了表征.分别研究了它们对六种指示菌的抑制作用并通过紫外吸收光谱对配合物与DNA的相互作用进行了研究.结果发现上述配合物对DNA的双螺旋结构产生了影响,并且对受试菌均有一定的抑制作用.

含二茂铁基Schiff碱及其金属配合物的合成、表征及抑菌活性

通过双乙酰基二茂铁和水合肼合成双乙酰基二茂铁双肼腙配体,然后分别与Cu(Ⅱ),Ni(Ⅱ),Zn(Ⅱ),Pb(Ⅱ),Cd(Ⅱ)合成金属配合物。配体及其金属配合物通过摩尔电导、元素分析、IR和1HNMR进行了表征。所有化合物进行了抗菌活性测试,结果表明,化合物都具有一定的抗菌活性,金属配合物2a^2f比其配体有更高的抗菌活性,其中,CdL(CH3COO)2(2f)的抗菌活性最高。

5-氯甲基水杨醛缩苯丙氨酸过渡金属(Ⅱ)配合物的合成及抗菌活性

在乙醇溶剂中合成5-氯甲基水杨醛缩苯丙氨酸新型Schiff碱配体及其过渡金属M(M=Mn2+、Co2+、Ni2+、Cu2+、Zn2+)配合物.通过元素分析、摩尔电导、红外光谱、紫外光谱及差热-热重方法对其组成和结构进行了表征.采用滤纸片法和试管二倍稀释法试验测定了Schiff碱及其过渡金属配合物对大肠埃希菌Escherichia coli和金黄色葡萄球菌Staphylococcus aureus的抗菌活性.结果表明Schiff碱配体为1∶1型电解质,其组成为KHL.H2O(L=C17H14O3NCl2-);合成的5种Schiff碱金属配合物均为非电解质类型,组成为[ML(H2O)].nH2O,配体L中的亚胺基氮、酚基氧、羧基氧均与中心金属离子M配位,另有1个水分子参与配位.荧光光谱试验显示,5种配合物的荧光强度均较相应Schiff碱配体的明显增强,其中锌配合物的荧光强度最大.体外抗菌试验结果表明该Schiff碱配体及其过渡金属配合物都具有一定的抗菌活性,而且配合物的抗菌活性强于Schiff碱配体,其中铜配合物对大肠埃希菌和金黄色葡萄球菌均表现出最强的抗菌能力,其对这2种细菌的最低抑菌浓度(MIC)分别为25.0和12.5μg.mL-1.

3,5-二碘水杨醛缩水杨酰肼Schiff碱及其金属配合物的合成与抑菌活性

以吡啶、DMF为溶剂合成了3,5-二碘水杨醛缩水杨酰肼Schiff碱的过渡金属配合物,用紫外可见光谱、红外光谱、TG-DTA、元素分析及摩尔电导率对配合物进行了表征,推测了配合物的可能结构,并对结构特征进行了分析。应用紫外光谱和荧光光谱测定方法研究了配合物与ct-DNA的作用,发现这些配合物均以插入方式与ct-DNA作用。另外,对各配合物作了活性测试,发现它们对阴离子超氧自由基O2-.和藤黄微球菌有良好的抑制作用。

2-胺乙基苯并咪唑金属配合物的合成、表征和抑菌活性研究

合成了2-胺乙基苯并咪唑(AEB)及M-AEB配合物(M=Cu2+、Ni2+或Co2+),通过元素分析、摩尔电导率、红外和紫外-可见光谱等进行了结构表征.结果表明:AEB通过咪唑N和胺基N以双齿形式与中心金属离子配位,配合物的分子组成式分别为:[Cu(AEB)2Cl]Cl(配合物1)、[Ni(AEB)3]Cl2(配合物2)和[Co(AEB)3]Cl2(配合物3).采用平皿滤纸片法测定了3种配合物对大肠埃希菌Escherichia coli、金葡萄球菌Staphylococcus aureus、枯草杆菌Bacillus subtilis和苏云金杆菌B.thuringiensis的抑菌活性.抑菌试验表明:在试验浓度下,配体AEB均没有抑菌活性,而与M配位后,在中、高试验浓度时表现出一定的抑菌活性,说明配合物中M的引入提高了AEB的抑菌活性.