Synthesis, characterisation, DNA binding, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities and molecular docking studies of metal(II) complexes with 1,10-phenanthroline scaffold.

A series of metal complexes containing Phenanthroline scaffold [ML] (L-1,10-Phenanthroline derivative comprises conjugated aromatic core and selenol group); M = Cu(II), Zn(II), Co(II) and Zn(II) ions were designed and synthesised to obtain effective anti-cholinesterase efficiencies of metal chelates. Analytical and spectroscopic studies were used to determine the structural features. An octahedral structure with moderate distortion was attributed to the above metal chelates based on spectroscopic data. The distorted octahedral geometry of copper(II) complex to DNA (Kb = 4.05 × 105 M-1) is stronger than that of ethidium bromide (EB) to DNA (Kb = 3.2 × 105 M-1), other metal complexes, respectively. The synthesised 1,10-Phenanthroline derivative had the best inhibitory effects against acetylcholinesterase (AChE) and butyrylcholinesterase, with IC50 values of 0.45 and 3.6 M, respectively, which were lower than the reference molecules. As a result, nitrogen-containing heterocyclic compounds (H2L) showed significant inhibitory profiles against the metabolic enzymes. Therefore, we believe that these experimental results may contribute to the development of new drug molecules particularly in the treatment of neurological disorders including glaucoma, Alzheimer's disease (AD) and diabetes. Docking, AChE and BuChE inhibition activities results revealed that ligand may be used for AD. The prepared 1,10-phenanthroline analogue, which has a high selectivity for AChE, may be studied further to find potential candidates for treating early-stage Alzheimer's symptoms.Communicated by Ramaswamy H. Sarma.

Synthesis, structural elucidation, DNA binding, cleavage, AChE and BuChE cholinesterase efficiencies of metal complexes with 1,10-phenanthroline scaffold.

A series of metal complexes containing a 1,10-phenanthroline scaffold [ML] (L-1,10-Phenanthroline derivative comprises conjugated aromatic core and electron withdrawing -NO2 group); M = Cu(II), Zn(II), Co(II), and Zn(II) ions were designed and synthesized to obtain effective anti-cholinesterase efficiencies of metal chelates. Analytical and spectroscopic studies were used to determine the structural features. An octahedral structure with moderate distortion was attributed to the above metal chelates based on spectroscopic data. S. aureus, A. niger, C. albicans, B.subtilis, A. flavus, and E. coli were used to test the antibacterial efficacy of the synthesized ligands and metal complexes. Using agarose gel electrophoresis, the DNA fragmentation proficiency of prepared metal complexes was tested on pUC 18 DNA. The distorted octahedral geometry of the copper(II) complex to DNA (Kb = 4.11 × 105 M-1) is stronger than that of ethidium bromide (EB) to DNA (Kb = 3.3 × 105 M-1) and other metal complexes, respectively. The synthesized 1,10-phenanthroline derivative had the best inhibitory effects against acetylcholinesterase and butyrylcholinesterase, with IC50 values of 0.45 and 3.6 M, respectively, which were lower than the reference molecules. Our experimental results may contribute to the development of new drug molecules particularly in the treatment of neurological disorders including glaucoma, Alzheimer's disease and diabetes. The actions of inhibitors on the glycosidase enzyme help to delay the breakdown and release of sugar molecules into the bloodstream, and they can be used as therapeutic factors in the treatment of diabetes.

Synthesis and in vitro biochemical properties, DNA binding and DNA cleavage ability of copper complexes of hydroxyflavone derivatives of novel organosulfur compounds as therapeutic agent.

Novel and synthetically essential flavonoids compounds containing the organosulfur moiety from Schiff bases, as well as their copper complexes, were synthesized from chrysin and 2-(phenylthio)aniline. These complexes were characterized using elemental analysis, mass spectrometry, electronic absorption spectroscopy, IR, 1H, and 13C NMR spectroscopy techniques. All the Cu(II) complexes exhibit square planar geometry. The in vitro antimicrobial activities of the investigated compounds were tested against the bacterial species, Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Staphylococcus epidermidis, and Klebsiella pneumoniae and fungal species, Aspergillus niger, Fusarium solani, Culvularia lunata, Rhizoctonia bataicola, and Candida albicans by serial dilution method. The DNA binding and DNA cleavage properties of copper complexes were studied. Free radical scavenging, superoxide dismutase, glutathione peroxidase, and antioxidant activities of the copper complexes have also been studied. In addition, using the egg albumin process, the in vitro anti-inflammatory efficacy of metal chelates was examined. Anti-tuberculosis and α-glucosidase inhibition activity were carried out from the prepared metal complexes. The flavonoid compounds containing the organosulfur moiety of Cu(II) complexes (1-8) exhibited better therapeutic agent.

Synthesis, characterization and pharmacological studies of copper complexes of flavone derivatives as potential anti-tuberculosis agents.

Novel series of different hydroxyflavone derivatives and their copper complexes were synthesized. They were characterized using analytical and spectral techniques. The superoxide dismutase (SOD) mimetic activity of the synthesized complexes demonstrated that copper complex of L(10) has promising SOD-mimetic activity than other ligands & complexes. The in vitro antimicrobial activities of the synthesized compounds were tested against the bacterial species and fungal species. The DNA binding properties of copper complexes were studied using cyclic voltametry and electronic absorption techniques. Anti-tuberculosis activity was also performed. The effective complexes was subjected to antimycobacterial activity using MABA method and summarized. The antimycobacterial activity of copper complexes have been evaluated and discussed.

Novel metal based anti-tuberculosis agent: synthesis, characterization, catalytic and pharmacological activities of copper complexes.

Copper complexes of molecular formulae, [CuL(1)(OAc)], [CuL(2)(H(2)O)], [CuL(3)(H(2)O)], [CuL(4)(H(2)O)], [CuL(5)(H(2)O)] where L(1)-L(5) represents Schiff base ligands [by the condensation of 3-hydroxyflavone with 4-aminoantipyrine (L(1))/o-aminophenol (L(2))/o-aminobenzoic acid (L(3))/o-aminothiazole (L(4))/thiosemicarbazide (L(5))], have been prepared. They were characterized using analytical and spectral techniques. The DNA binding properties of copper complexes were studied using electronic absorption spectra and viscosity measurements. Superoxide dismutase and antioxidant activities of the copper complexes have also been studied. Furthermore, the copper complexes have been found to promote pUC18 DNA cleavage in the presence of oxidant. Anti-tuberculosis activity was also performed.

Novel copper-based therapeutic agent for anti-inflammatory: synthesis, characterization, and biochemical activities of copper(II) complexes of hydroxyflavone Schiff bases.

Four hydroxyflavone derivatives have been synthesized with the aim of obtaining a good model of superoxide dismutase. Better to mimic the natural metalloenzyme, copper complexes have been designed. The Cu(II) complexes of general formulae, [CuL] where L = 5-hydroxyflavone-o-phenylenediamine (L¹H2)/m-phenylenediamine (L²H2) and 3-hydroxyflavone-o-phenylenediamine (L³H2)/m-phenylenediamine (L4H2) have been synthesized. The structural features have been determined from their analytical and spectral data. All the Cu(II) complexes exhibit square planar geometry. Redox behavior of copper complexes was studied and the present ligand systems stabilize the unusual oxidation state of the copper ion during electrolysis. The in vitro antimicrobial activities of the investigated compounds were tested against the bacterial species Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, and Pseudomonas aeruginosa and fungal species Aspergillus niger, Rhizopus stolonifer, Aspergillus flavus, Rhizoctonia bataicola, and Candida albicans. Superoxide dismutase and anti-inflammatory activities of the copper complexes have also been measured and discussed.