scholarly journals Synthesis and Structural Studies of Cr(III), Mn(II) and Fe(III) Complexes ofN(2-Benzimidazolyl)acetylacetohydrazone

2011 ◽  
Vol 8 (1) ◽  
pp. 421-426
Author(s):  
G. H. Anuradha ◽  
A. V. Chandra Pal

The ligandN(2-benzimidazolyl)acetylacetohydrazone (BAAH) have been synthesized and characterized. Coordination complexes of Cr(III), Mn(II) and Fe(III) have been synthesized with the ligand BAAH. These complexes were characterized on the basis of analytical, conductance, thermal, magnetic data and infrared and electronic spectral data. The ligand BAAH is behaving as a neutral tridentate NNO donar employing two azomethine nitrogens (ring and side chain) and carbonyl oxygen. The ligand and it's metal complexes were tested for anti microbial activity on the gram positiveS. Aureus, E. coliandProteus.

2009 ◽  
Vol 6 (1) ◽  
pp. 99-105 ◽  
Author(s):  
Prashant Singh ◽  
Shanu Das ◽  
Rajesh Dhakarey

Complexes of Co(II) with two new Schiff bases TEAB [2-hydroxy-4-{[2-oxo-2-(thiophen-2-yl)ethylidene]amino}benzoic acid] and TEPC [N-[2-oxo-2-(thiophen-2-yl)ethylidene]pyridine-3-carboxamide] have been synthesized and characterized with the help of elemental analysis, magnetic, mass,1H-NMR,13C-NMR, IR and electronic spectral data. IR spectra manifest the coordination of the ligand to the metal ion through the carbonyl oxygen, azomethine nitrogen and thienyl sulphur atoms. With the help of electronic spectral data various ligand field parameters were also calculated. All these studies reveal the distorted octahedral Co(II) complexes. Synthesized compounds have also been screened against some micro organismsviz, Escherichia coli, Proteus vulgaris, Aspergillus nigerandAspergillus flavuswith the help of ‘filter paper disc’ technique. It has been observed that the antimicrobial activities of metal complexes are higher than that of the free ligand.


1976 ◽  
Vol 29 (1) ◽  
pp. 79 ◽  
Author(s):  
PP Singh ◽  
UP Shukla ◽  
AK Srivastava

Coordination complexes of the type [CoL2] X2 (L = thiohydantoin (thn), pseudothiohydantoin (pthn); X = Cl, Br, I), [Ni(thn)4] Cl, and [Co(pthn)6] (ClO4), have been prepared and characterized by elementary analysis. The sites of bonding in ligands and configuration of the complexes have been determined with the help of physical properties, magnetic data, conductance data, i.r. and electronic spectral studies. The site of bonding in thn is thiocarbonyl sulphur and in pthn carbonyl oxygen. The cobalt halide complexes of thn and pthn are tetrahedral with C2v symmetry, [Ni(thn)4] Cl2 is octahedral with D4h symmetry and [Co(pthn)6] (ClO4), is octahedral with Oh cubic symmetry. All complexes except [Co(pthn)6] (ClO4)2, which is a 1 : 2 electrolyte, are non-conducting.


2011 ◽  
Vol 8 (1) ◽  
pp. 29-36 ◽  
Author(s):  
M. Neelamma ◽  
P. Venkateswar Rao ◽  
G. H. Anuradha

Transition metal complexes of Cr(III), Fe(III), Mn(II), Co(II), Ni(II), Cu(II) and Zn(II) with a tridentate ligand, 4-hydroxy-4-methyl-2-pentanone-1H-benzimidazole-2yl-hydrazone (H-HPBH) derived from the condensation of 2-hydrazinobenzimidazole and diacetone alcohol was synthesized. Characterization has been done on the basis of analytical, conductance, thermal and magnetic data, infrared,1H NMR, electronic, mass and ESR spectral data. From analytical and thermal data, the stoichiometry of the complexes has been found to be 1:1 (metal: ligand). Divalent complexes have the general formula [M(HPBH)Cl(H2O)2] in octahedral geometry, [M(HPBH)Cl] in tetrahedral and square planar stereochemistries and trivalent complexes [M(HPBH)Cl2(H2O)] in octahedral disposition. Infrared spectral data suggest that the ligand HPBH behaves as a monobasic tridentate ligand with N: N: O donor sequence towards the metal ions. On the basis of the above physicochemical data, octahedral, tetrahedral and square planar geometries were assigned for the complexes. The ligand and metal complexes were screened for their physiological activities againstE. coliandS. aureus. The order of physiological activity has been found to be Cu(II) > Ni(II) > Zn(II) > Co(II) > Cr(III) > Mn(II) > Fe (III) > ligand againstE.coliand Ni(II) > Cu(II) > Zn(II) > Mn(II) > Cr(III) > Fe(III) > Co(II) > ligand againstS. aureus.


Author(s):  
James A. Lake

The understanding of ribosome structure has advanced considerably in the last several years. Biochemists have characterized the constituent proteins and rRNA's of ribosomes. Complete sequences have been determined for some ribosomal proteins and specific antibodies have been prepared against all E. coli small subunit proteins. In addition, a number of naturally occuring systems of three dimensional ribosome crystals which are suitable for structural studies have been observed in eukaryotes. Although the crystals are, in general, too small for X-ray diffraction, their size is ideal for electron microscopy.


Author(s):  
Tahmeena Khan ◽  
Rumana Ahmad ◽  
Iqbal Azad ◽  
Saman Raza ◽  
Seema Joshi ◽  
...  

Background: Mixed ligand-metal complexes are efficient chelating agents because of flexible donor ability. Mixed ligand complexes containing hetero atoms sulphur, nitrogen and oxygen have been probed for their biological significance. Objective: Nine mixed ligand-metal complexes of 2-(butan-2-ylidene) hydrazinecarbothioamide (2-butanone thiosemicarbazone) and pyridine, bipyridine or 2-picoline as co-ligands were synthesized with Cu, Fe and Zn. The complexes were tested against MDA-MB231 (MDA) and A549 cell lines. Antibacterial activity was tested against S. aureus and E. coli. The drug character of the complexes was evaluated on several parameters viz. physicochemical properties, bioactivity scores, toxicity assessment and absorption, distribution, metabolism, excretion and toxicity (ADMET) profile assessment using various automated softwares. Molecular docking of the complexes was also performed with two target proteins. Method and Results: The mixed ligand-metal complexes were synthesized by condensation reaction for 4-5 h. The characterization was done by elemental analysis, 1H-NMR, FT-IR, molar conductance and UV spectroscopies. Molecular docking was performed against ribonucleotide reductase (RR) and topoisomerase II (topo II). [Cu(C5H11N3S)(py)2(CH3COO)2], [Zn(C5H11N3S)(bpy)(SO4)] and [Zn(C5H11N3S)(2-pic)2(SO4)] displayed the lowest binding energies with respect to RR. Against topo II [Cu(C5H11N3S)(py)2(CH3COO)2], [Cu(C5H11N3S)(bpy)(CH3COO)2] and [Zn(C5H11N3S)(2-pic)2(SO4)] had the lowest energies. The druglikness assessment was done using Leadlikeness and Lipinski’s rules. Against topo II [Cu(C5H11N3S)(py)2(CH3COO)2], [Cu(C5H11N3S)(bpy)(CH3COO)2] and [Zn(C5H11N3S)(2-pic)2(SO4)] had the lowest energies. Not more than two violations were obtained in case of each filtering rule showing drug like character of the mixed ligand complexes. Several of the complexes exhibited positive bioactivity scores and almost all the complexes were predicted to be safe with no hazardous effects. All the complexes were predicted to have no mutagenic character as shown by the Ames test [Zn(C5H11N3S)(py)2(SO4)] showed potential activity against MDA. [Co(C5H11N3S(bpy)(Cl)2] was also active against MDA. [Cu(C5H11N3S)(2-pic)2(CH3COO)2] also showed 27.6% cell viability at 100 µM against MDA. Against A549 [Co(C5H11N3S)(py)2(Cl)2], [Cu(C5H11N3S)(py)2(CH3COO)2] and [Co(C5H11N3S(bpy)(Cl)2] were active. [Co(C5H11N3S)(bpy)(Cl)2] and [Cu(C5H11N3S)(2-pic)2(CH3COO)2] were active against S. aureus. [Co(C5H11N3S)(2-pic)2(Cl)2] and [Zn(C5H11N3S)(2-pic)2(SO4)] were active at lower concentrations against S.aureus. Against E. coli, [Zn(C5H11N3S)(2-pic)2(SO4)] showed activity at 18-20mg dose range.


Antibiotics ◽  
2021 ◽  
Vol 10 (4) ◽  
pp. 418
Author(s):  
Shelley M. Horne ◽  
Angel Ugrinov ◽  
Birgit M. Prüβ

β-Phenylethylamine hydrochloride (PEA-HCl) and ethyl acetoacetate (EAA) are anti-microbials with applications in food processing. As food anti-microbials, the compounds will have to withstand the cooking process without changing to toxic compounds. With this Communication, we address the question of whether PEA and EAA are altered when heated to 73.9 °C or 93.3 °C. A combination of gas chromatography and mass spectrometry was used to analyze solutions of PEA(-HCl) or EAA in beef broth or water. In addition, the anti-microbial activity of PEA-HCl and EAA was compared between heated and unheated samples at a range of concentrations. The gas chromatograms of PEA(-HCl) and EAA showed one peak at early retention times that did not differ between the heated and unheated samples. The mass spectra for PEA and EAA were near identical to those from a spectral database and did not show any differences between the heated and unheated samples. We conclude that PEA(-HCl) and EAA formed pure solutions and were not altered during the heating process. In addition, the anti-microbial activity of PEA-HCl and EAA did not change after the heating of the compounds. Regardless of temperature, the minimal inhibitory concentrations (MICs) for PEA-HCl were 20.75 mmol mL−1 for Escherichia coli and Salmonella enterica serotype Typhimurium. For EAA, the MICs were 23.4 mmol mL−1 for E. coli and 15.6 mmol mL−1 for S. enterica.


2005 ◽  
Vol 49 (1) ◽  
pp. 281-288 ◽  
Author(s):  
Liqun Xiong ◽  
Yakov Korkhin ◽  
Alexander S. Mankin

ABSTRACT Ketolides represent the latest group of macrolide antibiotics. Tight binding of ketolides to the ribosome appears to correlate with the presence of an extended alkyl-aryl side chain. Recently developed 6,11-bridged bicyclic ketolides extend the spectrum of platforms used to generate new potent macrolides with extended alkyl-aryl side chains. The purpose of the present study was to characterize the site of binding and the action of bridged macrolides in the ribosomes of Escherichia coli. All the bridged macrolides investigated efficiently protected A2058 and A2059 in domain V of 23S rRNA from modification by dimethyl sulfate and U2609 from modification by carbodiimide. In addition, bridged macrolides that carry extended alkyl-aryl side chains protruding from the 6,11 bridge protected A752 in helix 35 of domain II of 23S rRNA from modification by dimethyl sulfate. Bridged macrolides efficiently displaced erythromycin from the ribosome in a competition binding assay. The A2058G mutation in 23S rRNA conferred resistance to the bridged macrolides. The U2609C mutation, which renders E. coli resistant to the previously studied ketolides telithromycin and cethromycin, barely affected cell susceptibility to the bridged macrolides used in this study. The results of the biochemical and genetic studies indicate that in the E. coli ribosome, bridged macrolides bind in the nascent peptide exit tunnel at the site previously described for other macrolide antibiotics. The presence of the side chain promotes the formation of specific interactions with the helix 35 of 23S rRNA.


2013 ◽  
Vol 639 (12-13) ◽  
pp. 2216-2223 ◽  
Author(s):  
Michael I. Bruce ◽  
Marcus L. Cole ◽  
Karine Costuas ◽  
Benjamin G. Ellis ◽  
Kathy A. Kramarczuk ◽  
...  

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