Heterocyclic Ligands Research Articles

Cytotoxic activity and influence on acetylcholinesterase of series dinuclear platinum(II) complexes with aromatic nitrogen-containing heterocyclic bridging ligands: Insights in the mechanisms of action

Herein, the stability, lipophilicity, in vitro cytotoxicity, and influence on acetylcholinesterase of five dinuclear platinum(II) complexes with the general formula [{Pt(en)Cl}2(μ-L)]2+ (L is a different aromatic nitrogen-containing heterocyclic bridging ligands pyrazine (pz, Pt1), pyridazine (pydz, Pt2), quinoxaline (qx, Pt3), phthalazine (phtz, Pt4) and quinazoline (qz, Pt5), while en is bidentate coordinated ethylenediamine) were evaluated. The most active analyzed platinum complexes induced time-dependent growth inhibition of A375, HeLa, PANC-1, and MRC-5 cells. The best efficiency was achieved on HeLa and PANC-1 cells for Pt1, Pt2, and Pt3 at the highest concentration, while Pt1 was significantly more potent than cisplatin at a lower concentration. Additionally, a lower effect on normal cells was observed compared to cisplatin, which may indicate potentially fewer side effects of these complexes. Selected complexes induce reactive oxygen species and apoptosis on tumor cell lines. The most potent reversible acetylcholinesterase (AChE) inhibitors were Pt2, Pt4, and Pt5. Pt1 showed similar inhibitory potential toward AChE as cisplatin, but a different type of inhibition, which could contribute to lower neurotoxicity. Docking studies revealed that Pt2 and Pt4 were bound to the active gorge above the catalytic triad. In contrast, the other complexes were bound to the edge of the active gorge without impeding the approach to the catalytic triad. According to this, Pt1 represents a promising compound with potent anticancer properties, high selectivity, and low neurotoxicity.

Heamanetic Effects of a Dioxidovanadium(V) Complex in STZ-Induced Diabetic Male Sprague Dawley Rats.

BackgroundDespite the effective maintenance of glucose homeostasis by insulin in type 1 diabetes mellitus, the drug has been implicated as one of the causes of haematological disturbances, which give rise to cardiovascular complications. As a result, research into alternative therapies for diabetes is needed. In our laboratory, an anti-hyperglycaemic novel vanadium complex has been synthesized using organic heterocyclic ligands. The complex has been shown and improve glycaemic control. The effects of this complex on haematological function, however, have not yet been established. Therefore, this study sought to investigate the haematological effects of dioxidovanadium(V) complex in (STZ)-induced diabetic rats.MethodsDiabetic rats received vanadium complex (40 mg kg −1 p.o), diabetic untreated (H2O) and insulin treated (0.175 mg kg−1 s.c), groups acted as a negative and positive control, respectively. Vanadium complex was administered twice daily, and blood glucose concentration was monitored weekly for 5 weeks. Thereafter, the animals were sacrificed followed by blood and kidneys collection for haematological (full blood count and Annexin V), hormonal (EPO) and oxidative status (SOD and GPx) analysis.ResultsAfter 5 weeks, untreated diabetic rats presented with hyperglycaemia compared to non-diabetic rats which was attenuated by vanadium complex administration. Furthermore, vanadium treated groups presented with an augmented RBC count, haematocrit, haemoglobin concentration, MCHC, MCV, and (EPO) levels compared to diabetic control. An increase in annexin V expression hence cell survival was observed in vanadium complex treated rats. Lastly, the administration of the complex improved antioxidant status as evidenced by increases in SOD and GPx concentration in plasma and in the kidneys.ConclusionThe administration of the anti-hyperglycaemic dioxidovanadium(V) complex improved haematological parameters, cell survival and the antioxidant status displayed by the diabetic rats. These results give an indication that the complex might be an effective alternative therapeutic drug for the treatment of hyperglycaemia in DM.

Specific features of sorption of bovine serum albumin on hydroxyapatite doped with zinc ions, and the possibilities of its use as an intermediate binding protein for heterocyclic ligands

Specific features of sorption of bovine serum albumin on hydroxyapatite doped with zinc ions, and the possibilities of its use as an intermediate binding protein for heterocyclic ligands

Halloysite Nanoclay with High Content of Sulfonic Acid-Based Ionic Liquid: A Novel Catalyst for the Synthesis of Tetrahydrobenzo[b]pyrans

One of the main drawbacks of supported ionic liquids is their low loading and consequently, low activity of the resultant catalysts. To furnish a solution to this issue, a novel heterocyclic ligand with multi imine sites was introduced on the surface of amino-functionalized halloysite support via successive reactions with 2,4,6-trichloro-1,3,5-triazine and 2-aminopyrimidine. Subsequently, the imine sites were transformed to sulfonic acid-based ionic liquids via reaction with 1,4-butanesultone. Using this strategy, high loading of ionic liquid was loaded on halloysite nanoclay. The supported ionic liquid was then characterized with XRD, SEM, TEM, EDS, FTIR, BET, TGA and elemental mapping analysis and utilized as a metal-free Brønsted acid catalyst for promoting one-pot reaction of aldehydes, dimedone and malononitrile to furnish tetrahydrobenzo[b]pyrans. The catalytic tests confirmed high performance of the catalyst. Moreover, the catalyst was stable upon recycling.

Prolonged Luminescence Lifetime of a Dual Emissive Ruthenium Dipyridophenazine-Type Complex in Aprotic and Protic Solvents.

A recently reported ruthenium(II) complex bearing an extended dipyridophenazine ligand exhibits unusual long-lived dual emission at room temperature. In this study, the effect of the introduction of a methyl protecting group to the imidazole moiety of this ligand (L1, 11-methyl-11H-imidazo[4,5-i]dipyrido[3,2-a:2',3'-c]phenazine) on the photophysics of the respective ruthenium(II) complex [(tbbpy)2Ru(L1)]2+ (C1) is demonstrated by means of electrochemistry, UV/vis absorption and emission spectroscopy, as well as emission lifetime measurements, and transient absorption spectroscopy on the nanosecond time scale. At room temperature, C1 shows dual emission both in aprotic and in protic solvents with time constants of 1.1/34.2 and 1.2/8.4 μs, respectively. These lifetimes are assigned to the emission from 3MLCT and 3LC states. The introduction of the methyl group increases the lifetime of the 3LC state in C1 almost by a factor of 2 in acetonitrile solution compared to the previously reported compound. Accordingly, the newly introduced methyl group is described as a protecting group for the imidazole moiety of the heterocyclic ligand, which enables prolonged lifetimes of the dual emissive complex in protic solvents. The stabilization of the electronic structure is further underlined by the enhanced stability toward electrochemical reduction as evidenced by cyclic voltammetry.

Synthesis and anticancer activity of Pt(0)‐olefin complexes bearing 1,3,5‐triaza‐7‐phosphaadamantane and N‐heterocyclic carbene ligands

A series of Pt(0)‐η2‐olefin complexes bearing 1,3,5‐triaza‐7‐phosphaadamantane (PTA) or N‐heterocyclic carbenes are prepared following different synthetic strategies depending on the nature of coordinated alkene and spectator ligands. These new platinum(0) derivatives have been tested in vitro as anticancer agents toward three different tumor (human ovarian cancer A2780 and A2780cis and K562 myelogenous leukemia) and one non‐tumor (Hacat keratinocytes) cell lines, proving to be in several cases highly and selectively cytotoxic against ovarian cancer cells. Furthermore, this antiproliferative effect is associated with the activation of an apoptosis process.In particular, complexes equipped with PTA as spectator ligand give comparable IC50 values on A2780 (cisplatin sensitive) and A2780cis (cisplatin resistant) cell lines, indirectly proving that these new Pt(0) substrates act with a mechanism of action conceivably different from cisplatin. This hypothesis is also confirmed by the fact that our compounds, in contrast to cisplatin, are not able to promote erythroid‐differentiation activity on the K562 myelogenous leukemia cell line.

Synthesis, Characterization, DFT and Antibacterial, Azo Ligand Derived From 2-Amino pyrimidine With Antipyrine Mixed ligand Complexes involving 1,10- phenanthroline

A new heterocyclic ligand (1,5-dimethyl-2-phenyl-4-(pyrimidin-2- yldiazenyl)-1,2-dihydro-3H-pyrazol-3-one, was synthesized by the diazotization of 2- (chlorodiazenyl)pyrimidine, and coupling with antipyrine to produce a new azo dye in an alkaline alcoholic solution under optimized experimental conditions (Azo-pyrm-Ap) (pyrimidin-2-yldiazenyl) ligand. and react with 1,10-phenanthroline, Ferric(II), Cobalt(II), Nickel(II), Copper(II), Zink(II), and Merrcury(II) ions were used to build the structure of mixed-ligand Tatradentate complexes. They confirmed all that by 1H- NMR,UVevisb, Fesem, XRD (DSC-TG) thermal analysis, Inferred- IR Magnetic susceptibility, The(C.H and N) analysis, molar conductance, and atomic absorption are all examples of spectroscopic techniques. The isolated solid complexes have been to have identified the formula in general [M (L)(phen) Cl] and [M (L)(phen)(H2O)] Cl, For prepared complexes, conductivity measurements revealed a [1:1] electrolyte. for Fe(II) and non-electrolyte for the Ni(II), Co(II), Zn(II), Cu(II), and, Hg(II) complexes. assemblages According to the spectral and analytical results, this ligand acts as a Bidentate chelating agent, with all metal ions having a coordination number of six. Finally, biological activity of the synthesized ligand and metal complexes against bacterial species was evaluated., Staphylococcus aureus is a Gram positive bacteria, and Escherichia coli, Pseudomonas aereuguinosa, and Klebsiella pneumoniaea are Gram negative bacteria. and it was found that these compounds have different inhibitory activity on bacteria growth.

Synthesis, spectral characterization, lethal dose (LD50) and acute toxicity studies of 1,4-Bis(imidazolylazo)benzene (BIAB)

The preparation and spectral identification of new heterocyclic azo ligand 1,4-Bis(imidazolylazo)benzene (BIAB) was prepared by reacting a diazonium chloride salt solution of 1,4-diaminobenzene with imidazole in alkaline ethanolic solution. Differing spectral techniques have been used to study the structure of the azo dye ligand (BIAB) such as Elemental analysis (C.H.N), 1H-NMR, Mass spectrum, UV-Vis, FT-IR, XRD, FE-SEM and thermal analysis (TGA-DTA). The pathogenic activities of the synthesized ligand (BIAB) was tested in vitro against the sensitive organisms Staphylococcus aureus (Gram-positive) and Escherichia coli (gram-negative) as antibacterial and Aspergillus Niger and Candida albicans as antifungal. The activity data show that the ligand (BIAB) higher antibacterial and slightly antifungus activity in comparison to the standard antibacterial (Amoxicillin) and antifungal (cycloheximide) drugs. The acute toxicity studies (LD50) was calculated using by Miller and Tainter methods (Estimated Probity Units) for the calculation of LD50. In this study, different doses (600, 1000, 1300, 1800, 2500 and 3600 μg/ml) of the (BIAB) was administered orally to the different groups of mice. The results exhibited high acute toxicity with LD50 of 1020.23 mg/kg upon intraperitoneal administration in mice. The antioxidant properties of the ligand was examined using the DPPH radical scavenging technique. IC50 was also determined at 224.17 μg/ml.

The Role of Counterions in Intermolecular Radical Coupling of Ru-bda Catalysts

Intermolecular radical coupling (also interaction of two metal centers I2M) is one of the main mechanisms for O–O bond formation in water oxidation catalysts. For Ru(bda)L2 (H2bda = 2,2′-bipyridine-6,6′-dicarboxylate, L = pyridine or similar nitrogen containing heterocyclic ligands) catalysts a significant driving force in water solution is the hydrophobic effects driven by the solvent. The same catalyst has been successfully employed to generate N2 from ammonia, also via I2M, but here the solvent was acetonitrile where hydrophobic effects are absent. We used a classical force field for the key intermediate [RuVIN(bda)(py)2]+ to simulate the dimerization free energy by calculation of the potential mean force, in both water and acetonitrile to understand the differences and similarities. In both solvents the complex dimerizes with similar free energy profiles. In water the complexes are essentially free cations with limited ion paring, while in acetonitrile the ion-pairing is much more significant. This ion-pairing leads to significant screening of the charges, making dimerization possible despite lower solvent polarity that could lead to repulsion between the charged complexes. In water the lower ion pairing is compensated by the hydrophobic effect leading to favorable dimerization despite repulsion of the charges. A hypothetical doubly charged [RuVIIN(bda)py2]2+ was also studied for deeper understanding of the charge effect. Despite the double charge the complexes only dimerized favorably in the lower dielectric solvent acetonitrile, while in water the separated state is more stable. In the doubly charged catalyst the effect of ion-pairing is even more pronounced in acetonitrile where it is fully paired similar to the 1+ complex, while in water the separation of the ions leads to greater repulsion between the two catalysts, which prevents dimerization.Graphic

Can Superhalogen Ligand Make More Reactive Frustrated Lewis Pairs?

AbstractNew Frustrated Lewis Pairs (FLPs) are designed and are attempted to activate molecular hydrogen. The new FLPs are modeled by changing the ligands in the Lewis acid (LA) part of the TPFPB (Tris(pentafluorophenyl)borane) molecule. The modifications are done by replacing the phenyl group in TPFPB with three different aromatic heterocyclic ligands. The stability and reactivity of FLPs: [(C2BNSHF2)]3B−P(tBu)3, [(C2BNSF3)]3B−P(tBu)3 and [C2BNO(CN)3]3B−P(tBu)3 is analysed in terms of the dual descriptors, NBO/Hirshfeld charges, VDE, hardness (η) and electrophilicity (ω). Although all three modeled FLPs show their capability towards activating molecular hydrogen, the [C2BNO(CN)3]3B−P(tBu)3 shows better performance than the conventionally used FLP: (C6F5)3B−P(tBu)3.

Tuning the structure of disulfonated phenanthroline based ligands for effective separation of Am(III)/Eu(III) ions : A DFT investigation

The disulfonated N,N′-diphenyl-2,9-diamide-1,10-phenanthroline (DS-Ph-DAPhen) ligand, is recently added to the list of efficient water-soluble heterocyclic ligands for the separation of actinides from lanthanides in nuclear waste management. This ligand contains phenyl sulfonate group which improves the solubility in aqueous medium. To understand the role of sulfonate group in selective binding of Am3+ over Eu3+ ions, a systematic investigation is executed on the designed disulfonated N,N′-diethyl-N,N′-diphenyl-2,9-diamide-1,10-phenanthroline (DS-Et-Ph-DAPhen) ligands. Here, we provide insights into the nature of metal–ligand bond in ML(NO3)3 complexes [M = Am and Eu] to trace the origin of selectivity in the separation process using scalar relativistic ZORA/DFT calculations. The quantum theory of atoms in molecules (QTAIM) and energy decomposition analysis (EDA) are carried out to understand the stabilizing interactions and binding energies of these ML(NO3)3 complexes respectively. Results reveal that DS-Et-Ph-DAPhen ligands show preferential binding to Am3+ where MO bond length is shorter and stronger than that of MN bonds. Computed separation factors indicate that meta-substitution is most favourable for extraction. Overall this study brings out the importance of sulfonate group in the stripping of Am3+ from Eu3+ and will shed light on the structural role played by sulfonate moiety for the nuclear waste treatment.

Designing of emerald terbium (III) ions with β-ketocarboxylic acid and heterocyclic ancillary ligands for biological and optoelectronic applications.

A green and highly efficient grinding method was adopted to synthesize emerald terbium complexes with 1-cyclopropyl-6-fluro-4-oxo-7-piperazin-1-ylquinoline-3-carboxylic acid as the main organic ligand and 2,2'-bipyridyl, 1,10-phenanthroline, neocuproine, 5,6-dimethyl-1,10-phenanthroline and bathophenanthroline as ancillary ligands. Structural analysis of these complexes was executed via elemental, infrared and 1 H-nuclear magnetic resonance analysis, which confirmed that the ligand coordinated to the metal ion through β-ketone and hydroxyl groups of carboxylic acid. Thermal stability of these complexes was investigated by study of thermogravimetric/derivative thermogravimetric analysis. Photoluminescence properties were investigated by observing emission spectra (400-700 nm), excitation spectra (250-500 nm) and decay time curves for display devices. The emission spectra revealed that an intense peak at 545 nm was observed due to 5 D4 →7 F5 electronic transition, which is responsible for the emerald colour in synthesized complexes, under 353 nm ultraviolet light excitation. The energy band gap and refractive index were determined, which proclaimed the dormant applications of these complexes in semiconductors. Commission Internationale de l'éclairage colour coordinates confirmed that the emerald emission of these complexes lies in the green region. Furthermore, antioxidant, antimicrobial and antimalarial assays of these complexes were also investigated, which confirmed that these complexes are potent for antioxidant, antimicrobial and antimalarial activities.

Binding mode transformation and biological activity on the Ru(II)-DMSO complexes bearing heterocyclic pyrazolyl ligands

Three Ru(II)-DMSO complexes (1-3) containing 2-(3-pyrazolyl)pyridine (PzPy), 2-pyrazol-3-ylfuran (PzO), or 2-pyrazol-3-ylthiophene (PzS) ligand, were synthesized and characterized. The monodentate coordination of the heterocyclic pyrazolyl ligand (PzPy) with Ru(II) ion via N atom was confirmed by single crystal X-ray diffraction. Complex 1 could be converted to the known η2-bidentate PzPy complex cis(Cl), cis(S)-[RuCl2(PzPy)(DMSO)2] (4) under reflux conditions. The mechanism underlying binding mode transformation was studied by 1H NMR spectroscopy and density functional theory (DFT) calculations. The binding abilities of the complexes (1–4) with calf-thymus (CT) DNA and bovine serum albumin (BSA) were investigated using spectroscopic and molecular docking techniques. Among the four Ru(II) complexes, complexes 1 and 3 inhibited the long-term proliferation of human breast cancer cells, whereas complexes 2 and 4 did not inhibit their proliferation to a considerable extent. Interestingly, complexes 1 and 3 did not induce significant cell death but rather attenuated the clonogenicity of breast cancer cells by upregulating reactive oxygen species (ROS), endoplasmic reticulum (ER) and autophagic stress.

Aqueous soluble ‘N′ donor heterocyclic ligands for the mutual separation of Am3+ and Eu3+: Solvent extraction, flat sheet supported liquid membrane and hollow fiber microextraction studies

Preferential stripping of the trivalent actinide ions such as Am(III) from the organic extract containing a mixture of Am(III) and Eu(III) by a suitable separation method is one of the most challenging areas of research which can find application in the radioactive waste management scheme. In the present study, a comparative evaluation of aqueous soluble tetrasulphonated derivatives of bis-triazinyl pyridine (BTP, LI), bis-triazinyl bipyridine (BTBP, LII) and bis-triazinyl phenanthroline (BTPhen, LIII) was done for the preferential stripping of Am(III) from a mixture of Am(III)/Eu(III) in the N,N,N′,N′-tetra-n-octyl diglycolamide (TODGA) extract. The results obtained in the solvent extraction studies were used for setting up of flat sheet supported liquid membrane based separation systems where the feed phase contained 1 M HNO3 spiked with the 241Am and 152,154Eu radiotracers while the receiver phase contained 0.01 M solutions of the aqueous soluble complexing agents in the presence of 1 M HNO3. Analogous studies were carried out using polypropylene hollow fibers leading to micro extraction of both Am(III) and Eu(III) and preferential stripping of Am(III) where promising separation behavior was observed, especially in the cases of LI and LIII with the DF values of 66 and 72, respectively for Am3+ over Eu3+ along with >80% recovery of Am.

Synthesis, spectroscopic characterisation, corrosion inhibition studies and dyeing properties of lanthanide(III) complexes of 1-[(3-carboxyethyl-4,5-dimethylthiophen-2-yl)azo]-2-naphthol

Ligational behaviour of the heterocyclic ligand obtained by coupling of diazotized 2-amino-3-carboxyethyl-4,5-dimethylthiophene with β-naphthol towards some selected lanthanide(III) ions has been studied. Various spectral and physico-chemical techniques have been used to confirm the coordination sites of the ligand (HTAN) and its lanthanide(III) complexes. It has been observed that these ligands coordinate to the metal ions in a neutral tridentate fashion. Thermal stability of metal chelates and structural stability of the chelating agent has been studied by thermal analysis. As lanthanides and azo dyes are reported as good corrosion inhibitors we have examined the corrosion inhibition activities of HTAN and its metal complexes. Also dyeing properties of the azo dye and some of its selected complexes towards cotton fabrics has been evaluated, as the traditional application field of the synthetic azo dyes still remains in the textile industry.

Zn(II) carboxylates containing heterocyclic secondary ligands: synthesis and structure manifestation through DFT studies

New Zn(II) complexes (1–8) of general formula [Zn(R)2(L')2], where R = cinnamic acid (1–7), L' = 3-pyridine carboxamide (1), 2,2'-bipyridine (2), 3-pyridinecarbonitrile (3), 2-amino-5-(4-pyridinyl)-1,3,4-thiadiazole (4), 2-methylimidazole (5), 2-phenylimidazole (6), 2-imidazolidinethione (7) and for (8), R = acetic acid; L' = 2-amino-5-(4-pyridinyl)-1,3,4-thiadiazole)2, have been synthesized by a stoichiometric reaction between Zn(II) carboxylate(s) and the respective nitrogen-based ligands. The prepared compounds are analyzed by FTIR, NMR spectroscopy and single crystal X-ray diffraction techniques for their structural manifestations along with elemental analyses. The crystallographic data for 6 and 8 exhibit four-coordinated zinc having distorted tetrahedral molecular geometry. The thermogravimetric data demonstrate high stability of the compounds with gradual loss of acetate and thiadiazol fragments that ultimately lead to zinc oxide as the residual mass of 8. Quantum chemical calculations indicate that 7 is the softest in reactivity having the lowest band gap as determined from the energies of frontier molecular orbitals whereas 8 is highly polar with the highest dipole moment value of 12.61 D. The computational data are a complement to the success of the research.

Visible-light excitable Eu3+-induced hyaluronic acid-chitosan aggregates with heterocyclic ligands for sensitive and fast recognition of hazardous ions

Water-soluble luminescent lanthanide complexes that can be excited with visible light could enable rapid detection of toxic anions and cations in biological systems. Eu3+-induced hyaluronic acid-chitosan aggregates (EIHCA) can improve the stability, biocompatibility, efficiency, and light absorption of luminescent Eu3+ complexes. Visible-range excitation may avoid phototoxicity associated with overexposure to UV light in biological and ecological applications. In this work, we synthesized and characterized series of EIHCA complexes having three N-donor heterocyclic ligands: 2,9-dimethyl-4,7-diphenyl-1,10-phenanthroline (Dphen), 2,2′: 6′,2″-terpyridine (Tpy) and 1,10-phenanthroline monohydrate (Phen). These complexes possessed bright red fluorescence with a visible range excitation maximum. The photophysical properties of one formulation (we denote as EDL6) include fast quenching response (20 s) of the fluorescence, multi-selectivity, low limit of detection, and high quenching (Ksv) values, enabling selective, rapid and sensitive recognition of Cr2O72− and Fe3+ in aqueous solution. Furthermore, EDL6 exhibits cytocompatibility with mammalian cells that make these complexes promising biocompatible candidate as a safe replacement of organic fluorophores for fluorescence sensing applications. Thus, these new EIHCA complexes were successfully employed for the selective detection of hazardous materials in biological and aqueous environment samples.

Molecular complexes of polar basic amino acids (l-lysine, l-histidine) with nicotinic acid in water and buffer solution: A thermodynamic aspects

Interactions of the polar basic amino acids, l-lysine (Lys) and l-histidine (His), with heterocyclic ligand, nicotinic acid (NA), in pure water and in phosphate buffer solution (pH 7.4) were studied by calorimetry and densimetry. Under the experimental conditions chosen, thermodynamic parameters of complex formation (lgKc, ΔcG, ΔcH, ΔcS) as well as the hydration enthalpies of different ionized forms of amino acids have been calculated at 298.15 K. The stoichiometry of complexes between Lys/His and NA was determined. The affinity of Lys to binding with NA decreases with increasing pH, the association process being less favorable. The more efficient stabilization of complexes between His and NA was exhibited in buffer media than in water. The apparent molar volumes, partial molar volumes and partial molar volume of transfer of NA from pure solvent (water/buffer) to mixed amino acid solution at infinite dilution have been evaluated. Their values obtained are lower for aqueous solutions than buffer systems. The dependence of thermodynamic characteristics obtained on molecular structure, ionization and hydration state of the solutes was analyzed. The dominant types of driving forces in the complex formation process of polar basic amino acids (Lys, His) with nicotinic acid were found for water and buffer solution.

Synthesis, Characterization and Biological Activity of Heterocyclic Azo-Schiff Base Ligand derived from 2-Amino-5-methyl thiazol and some Transition Metal Ions

A new dye with a, heterocyclic azo-Schiff base has been produced,. synthesized is being studied 5-(((E)-4-(dimethylamino)benzylidene)amino)-2-((E)-(5-methylthiazol-2-yl)diazenyl) phenol (LH) fromareaction of 2-amino-5-methyl thiazole with (dimethylamino) benzaldehyde, 3-amino phenol. Azo-Schiff base ligand reacted and including some metal ions, such as Fe(II), Co (III), Ni(II) forming chelates complex. They characterized by various analytical techniques like UV-Visb, H1-NMR, 13C- NMR spectroscopic, Molar conductance, FT-IR, Mass spectra, X-ray and FESEM elemental analysis also, The mole ratio, according to spectral tests, is [M:L] for complexes was [1:2].. This study also included the biological activity in the case of sensitive species Antibacterials include Escherichia coli (gram negative), Streptococcus (gram positive), and Penicillium (fungal)..It has been noticed that some complexes are very effective against. Azo ligand and Co(III) Complex show cytotoxis action against human Breast cancer cell line. The findings suggested that it could be used as an anti-cancer drug in medicine and pharmacy.

Synthesis of Difluoroglycine Derivatives from Amines, Difluorocarbene, and CO2: Computational Design, Scope, and Applications

A three-component reaction (3CR) for the synthesis of difluoroglycine derivatives has been achieved using amines, difluorocarbene (generated in situ ), and the abundant, inexpensive, and non-toxic C1 source CO 2 . Various tert -amines and pyridine, (iso)quinoline, imidazole, thiazole, and pyrazole derivatives were incorporated, and the corresponding products were isolated in solid form without purification using column chromatography on silica gel. Detailed reaction profiles of the 3CR were obtained via computational analysis using DFT calculations, and the results critically suggest that simple ammonia is not applicable to this reaction. In addition, strongly supported by computational predictions, a new reagent that can generate difluorocarbene at 0 °C without any additives was discovered. Furthermore, radical substitution reactions of the obtained difluoroglycine derivatives under photoredox conditions, as well as a synthetic application as an N -heterocyclic carbene ligand are shown.