Biological Screening of a Novel Nickel (II) Tyrosine Complex

et al. 2015

Applied Organom Chemis

*Seven new copper(II) complexes of type [Cu(A)(L)]ÁH 2 O (A = sparfloxacin, ciprofloxacin, levofloxacin, gatifloxacin, pefloxacin, ofloxacin, norfloxacin; L = 5-[(3-chlorophenyl)diazenyl]-4-hydroxy-1,3-thiazole-2(3H)-thione) were synthesized and characterized using elemental and thermogravimetric analyses, and electronic, electron paramagnetic resonance (EPR), Fourier transform infrared and liquid chromatography-mass spectroscopies. Tetrahedral geometry around copper is assigned in all complexes using EPR and electronic spectral analyses. All complexes were investigated for their interaction with herring sperm DNA utilizing absorption titration (K b = 1.27-3.13 × 10 5 M À1) and hydrodynamic volume measurement studies. The studies suggest the classical intercalative mode of DNA binding. The cleavage reaction on pUC19 DNA was monitored by agarose gel electrophoresis. The results indicate that the Cu(II) complexes can more effectively promote the cleavage of plasmid DNA. The superoxide dismutase mimic activity of the complexes was evaluated by nitroblue tetrazolium assay, and the complexes catalysed the dismutation of superoxide at pH = 7.8 with IC 50 values in the range 0.597-0.900 μM. The complexes were screened for their in vitro antibacterial activity against five pathogenic bacteria. All the complexes are good cytotoxic agents and show LC 50 values ranging from 5.559 to 11.912 μg ml À1. All newly synthesized Cu(II) complexes were also evaluated for their in vitro antimalarial activity against Plasmodium falciparum strain (IC 50 = 0.62-2.0 μg ml À1).

Section: Methodsmentioning

confidence: 99%

Synthesis, spectral investigation and development of tetrahedral copper(II) complexes as artificial metallonucleases and antimalarial agents

Mehta

Gajera

et al. 2015

Applied Organom Chemis

“…After 24 h the number of survivals was counted (Meyer et al, 1982). A graph of log of concentration of samples was plotted against percentage of mortality of nauplii (Islam et al, 2007). The LC 50 value is the antilogarithm of [complex] corresponding to the 50% mortality.…”

Section: Bsla -In Vitro Cytotoxicity Assaymentioning

confidence: 99%

Synthesis of heterocyclic compounds and its applications

Arabian Journal of Chemistry

Karia

Vekariya

et al. 2019

The octahedral ruthenium(II) complexes [Ru(L n )(PPh 3 ) 2 Cl 2 ] [L n = biphenyl furanyl pyridine derivatives] were synthesized and characterized using LC-MS, IR spectroscopy, elemental analysis and magnetic measurements. Complexes show enhancement in antibacterial activity compared to free ligands. From the binding mode investigation by absorption titration and viscosity measurement, it is observed that complexes bind to DNA via intercalation and also complexes promote the cleavage of supercoiled pUC19 plasmid DNA. Cytotoxicity analysis shows 100% mortality of Brine shrimp after 48 h. ª 2015 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

“…The in vitro lethality test has been carried out using brine shrimp eggs i.e. 38,39,55 Brine shrimp eggs were hatched in a shallow rectangular plastic dish (22×32 cm), filled with artificial seawater, which was prepared with commercial salt mixture and double distilled water.…”

Section: Cytotoxicity-brine Shrimp Lethality Bioassaymentioning

confidence: 99%

Novel 1,3,4-oxadiazole motifs bearing a quinoline nucleus: synthesis, characterization and biological evaluation of their antimicrobial, antitubercular, antimalarial and cytotoxic activities

Ladani

2015

New J. Chem.

A series of quinoline based 1,3,4-oxadiazole derivatives 8a-l were synthesized by chloro-amine coupling reaction approach with different catalyst and solvents. The substituted 1,3,4-oxadiazole intermediates 7a-c were obtained from 2-sustituted-N-phenylhydrazinecarbothioamide 6a-c by cyclization with different cyclizing reagents like mercuric acetate, lead dioxide, iodobenzenediacetate (IBD) and aqueous sodium hydroxide with iodine in aqueous potassium iodide to isolate the most effective reaction condition by using iodobenzenediacetate as extremely good catalyst. The structure of the title compounds were confirmed by FT-IR, 1 H NMR, 13 C NMR and mass spectrometry. The synthesized molecules were evaluated for their antibacterial, antifungal, antituberculosis and antimalarial activities. The brine shrimp bioassay was carried out to study the in vitro cytotoxic properties for the highly active compounds of in vitro biological evaluation. antifungal 34 . Quinoline scaffolds have been selected due to their diverse therapeutic and pharmacological properties, such as antitumor, antiatherosclerotic, vasodilator, geroprotective, bronchodilator and hepatoprotective activity 35 .