Synthesis of Novel Phosphonic‐Type Activity‐Based Probes for Neutrophil Serine Proteases and Their Application in Spleen Lysates of Different Organisms

Neutrophils are a type of granulocyte important in the “first line of defense” of the innate immune system. Upon activation, they facilitate the destruction of invading microorganisms by the production of superoxide radicals, as well as the release of the enzymatic contents of their lysozymes. These enzymes include specific serine proteases: cathepsin G, neutrophil elastase, proteinase 3, as well as the recently discovered neutrophil serine protease 4 (NSP4). Under normal conditions, the proteolytic activity of neutrophil proteases is tightly regulated by endogenous serpins; however, this mechanism can be subverted during tissue stress, thereby resulting in the uncontrolled activity of serine proteases, which induce chronic inflammation and subsequent pathology. Herein, we describe the development of low‐molecular‐weight activity‐based probes that specifically target the active sites of neutrophil proteases.     

新型过渡金属配合物的合成、表征及生物活性研究

为了寻找更好的生物活性化合物,以1-苯基-3-甲基-5-吡唑啉酮和苯甲酰氯为原料,二氧六环为溶剂,回流反应合成了4-酰基吡唑啉酮配体及4种过渡金属配合物,通过元素分析、红外光谱、差热-热重分析、紫外光谱等对其结构进行了表征,表明配合物组成分别为:Cu(L)2、Zn(L)2、Ni(L)2、Mn(L)2;同时利用抑菌圈大小...     

Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors

A series of coumarin-thiadiazole hybrids and their corresponding Cu(II) and Zn(II) complexes were synthesized and characterized with the use of spectroscopic techniques. The results obtained indicate that all the coumarin-thiadiazole hybrids act as bidentate chelators of Cu(II) and Zn(II) ions. The complexes isolated differ in their ligand:metal ratio depending on the central metal. In most cases, the Zn(II) complexes are characteristic of a 1:1 ligand:metal ratio, while in the Cu(II) complexes the ligand:metal ratio is 2:1. All compounds were tested as potential antibacterial agents against Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacterial strains demonstrating activities notably lower than commercially available antibiotics. The more promising results were obtained from the assessment of antineurodegenerative potency as all compounds showed moderate acetylcholinesterase (AChE) inhibition activity     

Mn-SOD酶模拟化合物的合成、表征及活性检测

SOD在维持生物体内O-2.产生与消除的动态平衡中起着重要的作用,其小分子模拟化合物的研究一直受到重视,文章合成了一种模拟SOD的锰配合物,应用X射线衍射方法测定了其晶体结构,并对它们进行了红外光谱图、紫外光谱图表征,最后利用邻苯三酚自氧化法进行了生物活性检测。     

对-亚苯基双苯并咪唑过渡金属配合物的合成和荧光性质研究

合成了2,2’-对亚苯基双苯并咪唑的铜、钴、镍配合物,采用元素分析、红外光谱、紫外光谱和摩尔电导率等进行表征,研究了固体荧光性质,发现Ni（II）配合物的荧光发射峰红移了101nm,荧光寿命增加到配体的12倍。     

Synthesis and Characterization of Novel Polymeric-Schiff Bases and Their Complexes

An investigation of the solid state conductivity of polymeric-Schiff bases derived from the condensation reaction of polyacrylamide and an aldehyde (4-methoxybenzaldehyde and 4-chlorbenzaldehyde) has been carried out and Co(II) and Ni(II) complexes have been prepared. Polymeric-Schiff bases and their metal complexes were characterized by molar conductance, magnetic susceptibility, and electronic and IR spectral studies. Conductivity measurements were carried out at 20 °C in dimethylformamide to determine the electrolytic behavior. The ¹H-NMR and ¹³C-NMR spectra, elemental analysis, and viscosity average molecular mass (M _v) of the polymeric-Schiff bases and their complexes were determined. All of the polymer–metal complexes showed high thermally stability. The DC conductivities of the solid samples were measured using a four-probe technique.     

Synthesis, Spectral and Antibacterial Studies of Copper(II) Tetraaza Macrocyclic Complexes

A novel family of tetraaza macrocyclic Cu(II) complexes [CuLX(2)] (where L = N(4) donor macrocyclic ligands) and (X = Cl(-), NO(3) (-)) have been synthesized and characterized by elemental analysis, magnetic moments, IR, EPR, mass, electronic spectra and thermal studies. The magnetic moments and electronic spectral studies suggest square planar geometry for [Cu(DBACDT)]Cl(2) and [Cu(DBACDT)](NO(3))(2) complexes and distorted octahedral geometry to the rest of the ten complexes. The biological activity of all these complexes against gram-positive and gram-negative bacteria was compared with the activity of existing commercial antibacterial compounds like Linezolid and Cefaclor. Six complexes out of twelve were found to be most potent against both gram-positive as well as gram-negative bacteria due to the presence of thio group in the coordinated ligands.     

金属有机配合物的合成及晶体培养

金属有机配合物因具有独特的催化活性、光学特性、磁学性质和生物学性质等而受到人们的广泛关注。它们在磁性材料、发光材料、非线性光学材料、微孔材料的研制方面扮演着重要的角色。本文详细介绍了金属有机配合物的6种合成方法及它们各自的优缺点,总结出了晶体生长的几种关键因素并对各种因素进行了详细的分析。     

Synthesis,Crystallographic Structure,Theoretical Analysis,Molecular Docking Studies,and Biological Activity Evaluation of Binuclear Ru(II)-1-Naphthylhydrazine Complex

Ruthenium(II)–arene complexes have gained significant research interest due to their possible application in cancer therapy. In this contribution two new complexes are described, namely [{RuCl(η⁶-p-cymene)}₂(μ-Cl)(μ-1-N,N′-naphthyl)]X (X = Cl, 1; PF₆, 2), which were fully characterized by IR, NMR, and elemental microanalysis. Furthermore, the structure of 2 in the solid state was determined by a single crystal X-ray crystallographic study, confirming the composition of the crystals as 2·2MeOH. The Hirshfeld surface analysis was employed for the investigation of interactions that govern the crystal structure of 2·2MeOH. The structural data for 2 out of 2·2MeOH was used for the theoretical analysis of the cationic part [{RuCl(η⁶-p-cymene)}₂(μ-Cl)(μ-1-N,N′-naphthyl)]⁺ (2a) which is common to both 1 and 2. The density functional theory, at B3LYP/6-31+G(d,p) basis set for H, C, N, and Cl atoms and LanL2DZ for Ru ions, was used for the optimization of the 2a structure. The natural bond orbital and quantum theory of atoms in molecules analyses were employed to quantify the intramolecular interactions. The reproduction of experimental IR and NMR spectra proved the applicability of the chosen level of theory. The binding of 1 to bovine serum albumin was examined by spectrofluorimetry and molecular docking, with complementary results obtained. Compound 1 acted as a radical scavenger towards DPPH^• and HO^• radicals, along with high activity towards cancer prostate and colon cell lines.     

Cationic Peptides and Their Cu(II) and Ni(II) Complexes: Coordination and Biological Characteristics

Antimicrobial peptides are a promising group of compounds used for the treatment of infections. In some cases, metal ions are essential to activate these molecules. Examples of metalloantibiotics are, for instance, bleomycin and dermcidin. This study is focused on three new pseudopeptides with potential biological activity. The coordination behavior of all ligands with Cu(II) and Ni(II) ions has been examined. Various analytical methods such as potentiometric titration, UV-Vis and CD spectroscopies, and mass spectrometry were used. All compounds are convenient chelators for metal ion-binding. Two of the ligands tested have histidine residues. Surprisingly, imidazole nitrogen is not involved in the coordination of the metal ion. The N-terminal amino group, Dab side chains, and amide nitrogen atoms of the peptide bonds coordinated Cu(II) and Ni(II) in all the complexes formed. The cytotoxicity of three pseudopeptides and their complexes was evaluated. Moreover, their other model allowed for assessing the attenuation of LPS-induced cytotoxicity and anti-inflammatory activities were also evaluated, the results of which revealed to be very promising.     

含氮,硫有机配体及金属配合物的合成和生理活性研究

综述了国内外关于含氮、硫有机配体及金属配合物的合成和生理活性研究进展,同时介绍了作者在该方面的研究情况。     

Synthesis,Structure, Spectral-Luminescent Properties,and Biological Activity of Chlorine-Substituted N-[2-(Phenyliminomethyl)phenyl]-4-methylbenzenesulfamide and Their Zinc(II) Complexes

New azomethine compounds of 2-(N-tosylamino)benzaldehyde or 5-chloro-2-(N-tosylamino)benzaldehyde and the corresponding chlorine-substituted anilines, zinc(II) complexes based on them have been synthesized. The structures of azomethines and their complexes were determined by elemental analysis, IR, ¹H NMR, X-ray spectroscopy, and X-ray diffraction. It is found that all ZnL₂ complexes have a tetrahedral structure according to XAFS and X-ray diffraction data. The photoluminescent properties of azomethines and zinc complexes in methylene chloride solution and in solid form have been studied. It is shown that the photoluminescence quantum yields of solid samples of the complexes are an order of magnitude higher compared to the solutions and range from 11.34% to 48.3%. The thermal properties of Zn(II) complexes were determined by thermal gravimetric analysis (TGA) and differential scanning calorimetry. The TGA curves of all the compounds suggest their high thermal stability up to temperatures higher than 290 °C. The electrochemical properties of all complexes were investigated by the cyclic voltammetry method. The multilayered devices ITO/PEDOT:PSS/NPD/Zn complex/ TPBI/LiF/Al with wide electroluminescence (EL) color range spanning the range from bluish-green (494 nm) to green (533 nm) and the high values of brightness, current and power efficiency were fabricated. The biological activity of azomethines and zinc complexes has been studied. In the case of complexes, the protistocidal activity of the zinc complex with azomethine of 5-chloro-2-(N-tosylamino)benzaldehyde with 4-chloroaniline was two times higher than the activity of the reference drug toltrazuril.     

Synthesis, Spectroscopy and Electrochemistry of Fe(II) and Fe(III) Quinonemonooxime Complexes and Their DNA Cleaving Activities

Iron(II) and iron(III) complexes of 3,5-di-tert-butyl-o-benzoquinonemonooxime were synthesized and characterized by spectroscopic and electrochemical studies. Their ability to cleave DNA has been investigated under aerobic conditions at room temperature and in the presence and absence of H(2) O(2). The plasmid DNA pBR322 was effectively cleaved by these complexes in a concentration dependant manner.     

橙皮素及其席夫碱金属配合物的合成及性质研究

利用缩合反应,在无水乙醇中合成橙皮素金属配合物;橙皮素在无水乙醇(或异丙醇)中与苯胺生成席夫碱,用此席夫碱合成新的橙皮素席夫碱金属配合物,并对其结构进行了表征.     

新型双核席夫碱化合物的合成、表征

用乙二胺、乙酰丙酮与水杨醛反应合成了一种不对称席夫碱配体单元（H2L^1）,将所得不对称席夫碱配体单元（H2L^1）与氨水、I2反应合成了对称新型双核席夫碱配体（H4L^1）,通过元素分析、核磁共振、红外光谱、质谱分析、紫外光谱等手段对合成得到的不对称席夫碱配体单元及新型双核席夫碱化合物进行了表征。     

Metal Complexes with Schiff Bases: Data Collection and Recent Studies on Biological Activities

Metal complexes play a crucial role in pharmaceutical sciences owing to their wide and significant activities. Schiff bases (SBs) are multifaceted pharmacophores capable of forming chelating complexes with various metals in different oxidation states. Complexes with SBs are extensively studied for their numerous advantages, including low cost and simple synthetic strategies. They have been reported to possess a variety of biological activities, including antimicrobial, anticancer, antioxidant, antimalarial, analgesic, antiviral, antipyretic, and antidiabetic ones. This review summarizes the most recent studies on the antimicrobial and antiproliferative activities of SBs-metal complexes. Moreover, recent studies regarding mononuclear and binuclear complexes with SBs are described, including antioxidant, antidiabetic, antimalarial, antileishmanial, anti-Alzheimer, and catecholase activities.     

木犀草素Zn(II)和Cu(II)配合物的合成及电化学性质研究

在无水乙醇溶液中,用木犀草素和醋酸铜、醋酸锌合成两种鲜见报道的木犀草素金属配合物,并通过元素分析、红外光谱、电子光谱和摩尔电导等表征手段,确定了配合物的结构。并研究了木犀草素Zn(II)和木犀草素Cu(II)配合物化学修饰碳糊电极在pH 5 B-R缓冲溶液中的电化学行为。     

Spectroscopic Characterization and Biological Activity of Hesperetin Schiff Bases and Their Cu(II) Complexes

The three Schiff base ligands, derivatives of hesperetin, HHSB (N-[2,3-dihydro-5,7-dihydroxy-2-(3-hydroxy-4-methoxyphenyl)chromen-4-ylidene]isonicotinohydrazide), HIN (N-[2,3-dihydro-5,7-dihydroxy-2-(3-hydroxy-4-methoxyphenyl)chromen-4-ylidene]benzhydrazide) and HTSC (N-[2,3-dihydro-5,7-dihydroxy-2-(3-hydroxy-4-methoxyphenyl)chromen-4-ylidene]thiosemicarbazide) and their copper complexes, CuHHSB, CuHIN, and CuHTSC were designed, synthesized and analyzed in terms of their spectral characterization and the genotoxic activity. Their structures were established using several methods: elemental analysis, FT-IR, UV-Vis, EPR, and ESI-MS. Spectral data showed that in the acetate complexes the tested Schiff bases act as neutral tridentate ligand coordinating to the copper ion through two oxygen (or oxygen and sulphur) donor atoms and a nitrogen donor atom. EPR measurements indicate that in solution the complexes keep their structures with the ligands remaining bound to copper(II) in a tridentate fashion with (O^–, N, O_ket) or (O^–, N, S) donor set. The genotoxic activity of the compounds was tested against model tumour (HeLa and Caco-2) and normal (LLC-PK1) cell lines. In HeLa cells the genotoxicity for all tested compounds was noticed, for HHSB and CuHHSB was the highest, for HTSC and CuHTSC–the lowest. Generally, Cu complexes displayed lower genotoxicity to HeLa cells than ligands. In the case of Caco-2 cell line HHSB and HTSC induced the strongest breaks to DNA. On the other side, CuHHSB and CuHTSC induced the highest DNA damage against LLC-PK1.     

希夫碱金属配合物作为催化剂的应用

简要介绍了近几年来希夫碱及其金属配合物作为催化剂在催化氧化反应,烯烃的聚合、环丙烷化以及环氧化反应中的研究进展。     

二苯氨基修饰的阳离子型环金属铂(II)配合物的合成及性能

以1,10-邻菲罗啉为辅助配体，设计合成了三个二苯氨基修饰的阳离子型环金属铂(II)配合物Ⅰ-Ⅲ。系统研究了配合物的光物理、电化学及氧传感性能。结果表明，在2-(4-二苯氨基)苯基吡啶的吡啶环的5位引入不同基团，可实现铂(II)配合物的发光波长在544 nm - 583 nm之间调控。其中，在吡啶环的5位引入三氟甲基的配合物Ⅲ的最大发射波长为583 nm。氧传感性能测试结果表明，在吡啶环的5位引入三氟甲基的配合物Ⅲ的氧敏感性能显著提升，其在DMF溶液中的I0/I2.17值为6.4。