Synthesis, Characterization, and Antimicrobial and Antispermatogenic Activity of Bismuth(III) and Arsenic(III) Derivatives of Biologically Potent Nitrogen and Sulfur Donor Ligands (original) (raw)
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Transition Metal Chemistry, 2001
Complexes of S-benzyldithiocarbazate (SBDTC) with lighter and heavier metals, viz., CrIII, FeIII, SbIII, ZrIV, ThIV and UVI have been prepared and characterized by elemental analyses, conductivity measurements, and spectral studies. The complexes: [Cr(SBDTCA)3],** [Fe(SBDTCA)3], [Sb(SBDTCA)3], [Sb(SBDTCA)2Cl · H2O], [Zr(O)(SBDTCA)2 · H2O], [Th(SBDTCA)(NO3)3 · H2O)], and [U(O)2(SBDTCA)2] were all prepared in alkaline media. They were all hexa-coordinated with bidentate, uninegative chelation of the ligand. [Fe(SBDTCA)3], [Sb(SBDTCA)3] and [Sb(SBDTCA)2Cl · H2O] were strongly effective against bacteria giving clear inhibition zones with Pseudomonas aeruginosa and Bacillus cereus. The compounds showed poor antifungal activity. The antimony complexes were strongly cytotoxic against leukemic cells with CD50 values of 3.2–6.7 μg cm−3 as compared to the CD50 value of 14.5 μg cm−3 of the free SbCl3 molecule.
2014
New antibacterial and antifungal Schiff's base derived from substituted benzothiazoline (N C SH), as well as its main group metal complexes incorporating antimony(III), bismuth(III) and arsenic(III) were synthesized with conventional as well as microwave irradiation method, characterized and screened for their in-vitro antibacterial as well as antifungal activity against Gram-negative ( Escherichia coli ), Gram-positive ( Staphylococcus aureous ) microbial strains and Fusarium oxysporum and Aspergillus niger fungal strains. The metal complexes show more antimicrobial potency as compared to the uncomplexed Schiffs' base. The ligand and its BiCl(N C S) 2 and PhAs(N C S) 2 compounds have been screened in vivo in male albino rats to test their antifertility property and results indicated that the administration of aforesaid compounds in male rats brought about an interference with spermatogenesis which ultimately caused infertility
A novel Schiff base ligand N-(4-phenylthiazol-2yl)-2-((2-thiaxo-1,2-dihydroquinolin-3-yl)methylene)hydrazinecarboxamide (L) obtained by the condensation of N-(4-phenylthiazol-2-yl)hydrazinecarboxamide with 2-thioxo-1,2-dihydroquinoline-3- carbaldehyde and its newly synthesized Cu(II), Co(II), Ni(II), and Zn(II) complexes have been characterized by elemental analysis and various spectral studies like FT-IR, 1H NMR, ESI mass, UV-Visible, ESR, TGA/DTA, and powder X-ray diffraction studies. The Schiff base ligand (L) behaves as tridentate ONS donor and forms the complexes of type [ML(Cl)2] with square pyramidal geometry. The Schiff base ligand (L) and its metal complexes have been screened in vitro for their antibacterial and antifungal activities by minimum inhibitory concentration (MIC) method.The DNA cleavage activity of ligand and its metal complexes were studied using plasmid DNA pBR322 as a target molecule by gel electrophoresis method.The brine shrimp bioassay was also carried out to study the in vitro cytotoxicity properties for the ligand and its metal complexes against Artemia salina. The results showed that the biological activities of the ligand were found to be increased on complexation.
2013
Present thesis describes the synthesis, characterization and biological screening of sulfonamide ligands; their complexes and five membered heterocyclic ligands (Thiohydantoin ligands); their complexes aiming in search of new candidates to fight with microorganisms. Thanks to metals for being the charm of medicinal and pharmaceutical chemistry since many decades. To extend this search, 20 ligands were synthesized. Ligands containing sulfonamide moieties are prepared by the reaction of ten different amino acids with p-toluene sulfonyl chloride. The compounds are isolated in pure form and checked by TLC. The single crystal structure of the compounds is also reported and dicussed.These compounds were then reacted with transition metals e.g, Zn (II), Sb (III) chloride and Sb (III) bromide and thirty new metal complexes have been synthesized. Further, these sulfonamide derivatives were cyclized in the presence of NH4SCN, acetic anhydride and base to form 5-membered heterocyclic ring cont...
Molecules, 2013
Thirty two new Cu(II), Ni(II) and Zn(II) complexes (1-32) with salicylidene thiosemicarbazones (H 2 L 1 -H 2 L 10 ) were synthesized. Salicylidene thiosemicarbazones, of general formula (X)N-NH-C(S)-NH(Y), were prepared through the condensation reaction of 2-hydroxybenzaldehyde and its derivatives (X) with thiosemicarbazide or 4-phenylthiosemicarbazide (Y = H, C 6 H 5 ). The characterization of the new formed compounds was done by 1 H-NMR, 13 C-NMR, IR spectroscopy, elemental analysis, magnetochemical, thermoanalytical and molar conductance measurements. In addition, the structure of the complex 5 has been determined by X-ray diffraction method. All ligands and metal complexes were tested as inhibitors of human leukemia (HL-60) cells growth and antibacterial and antifungal activities.
Molecules
Four new complexes (Ni2+, Cu2+, Ag+, and Hg2+) were prepared from the ligand N-(4-chlorophenyl)-2-(phenylglycyl)hydrazine-1-carbothioamide (H2L). Analytical and spectroscopic techniques were used to clarify the structural composition of the new chelates. In addition, all chelates were tested against bacterial strains and the HepG2 cell line to determine their antiseptic and carcinogenic properties. The Ni(II) complex was preferable to the other chelates. Molecular optimization revealed that H2L had the highest reactivity, followed by Hg-chelate, Ag-chelate, Ni-chelate, and Cu-chelate. Moreover, molecular docking was investigated against two different proteins: the ribosyltransferase enzyme (code: 3GEY) and the EGFR tyrosine kinase receptor (code: 1m17).
Objective: The objective of this study is to synthesize Schiff's base ligands of thiosemicarbazone2-benzoyalpyridine and their copper complexes and study their antimicrobial activity. Materials and Method: Thiosemicarbazone2-benzoylpyridine Schiff's base ligand was prepared by reflux method by using ethyl alcohol as solvent for 7-8 hrs. Ligand under study was found to be highly soluble in water, and its complexes were prepared in water. P H was adjusted as per the requirement in each case (approximately 6-7). Round bottom flask (100 mL), condenser, and heating mental were used as apparatus. Result: The complexes of Cu(II) having the general composition CuL 2 X 2 (where L = 2-benzoylpyridine thiosemicarbazone and X = Cl-, NO 3-, ½SO 4 2-) have been synthesized. The complexes of Cu(II) under study were characterized by IR, elemental analysis, magnetic susceptibility, UV, molar conductivity, mass spectrometry, and electron EPR spectral studies. Molar conductance value was calculated using DMSO as solvent. The magnetic moment indicates that all the complexes were of high spin type. On the basis of spectral studies, an octahedral geometry has been proposed for Cu (II) complexes. The complexes under study were screened for antifungal (i.e., Candida krusei and Candida parapsilosis) and antibacterial (i.e., Escherichia coli and Staphylococcus) activities. Conclusion: The synthesized ligand was bidentate and their complexes were found more active toward antimicrobial activity than ligands.
Scholars international journal of chemistry and material sciences, 2023
The New ligand 5-methyl-2-(2-thienyl)-1,3-oxazole-4-carbaldehyde thiosemicarbazone (HL)(1) was synthesized. This ligand reacted with Co(II) and Ni(II) chloride in ratio 1:2 metal:ligand afforded two complexes, [Co(LH)]Cl 2 (2) and [Ni(HL) 2 ]Cl 2 (3). The ligand and its metal (II) complexes have been characterized by spectroscopic techniques. The Xray structural studies revealed that the free ligand exist in thione form and remain as neutral tridentate with NNS donor atoms in the tow complexes beside presence of uncoordinated chloride ions in the cavities of the crystal lattice of the complexes. One of these chlorides in complex (2) is hydrogen bonded to a proton of the amine of the ligand. While in complex (3) the chloride bonded to proton of imine (-N 2 H) of the ligand and the coordination environment has a distorted octahedral. The oxazole N and S atoms in the two complexes are cis to each other whereas the azomethine N atoms are trans coordinated. The ligand and its metal complexes were tested for their in vitro biological activity against six standard microorganisms: two Gram positive namely Bacillus subtilis and Micrococcus luteus, and one Gram negative bacteria Escherichia coli and three fungi: Saccharomyces cerevisiae (Baker's yeast), Mucor spec., and Aspergillus niger, at a concentration 100µg/ml.