scholarly journals Synthesis, spectral characterization, DNA interaction studies, anthelmintic and antimicrobial activity of transition metal complexes with 3-(2- hydroxybenzylideneamino)-2-methylquinazolin-4(3H)-one and 1,10- phenanthroline

2011 ◽  
Vol 1 (4) ◽  
pp. 127-138 ◽  

Mixed ligand complexes of cobalt(II) (1), copper(II) (2) and oxovanadium(IV) (3) with 3- (2-hydroxy benzylideneamino)-2-methylquinazolin-4(3H)-one and 1,10-phenanthroline have been synthesized and characterized by elemental analyses, IR, electronic, 1 H-NMR, mass spectra, molar conductance and thermal studies. The synthesized compounds were screened for their in vitro antimicrobial activity. The results show a significant increase in antimicrobial activity of the complexes compared to ligand. Antihelmintic activity of the compounds has been tested on earthworms and the enhanced activity was observed upon complexation. In addition, DNA binding and DNA cleavage studies for the newly prepared compounds were also studied. These studies indicate that the DNA binding and cleavage efficacy were increased in the complexes relative to the parental ligand.

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
S. Nagashree ◽  
P. Mallu ◽  
L. Mallesha ◽  
S. Bindya

A series of methyl-2-aminopyridine-4-carboxylate derivatives,3a–f,were synthesized in order to determine theirin vitroantimicrobial activity. The chemical structures of the synthesized compounds were confirmed by elemental analyses, FT-IR, and1H NMR spectral studies. Among the synthesized compounds,3cand3dshowed good antimicrobial activity compared to other compounds in the series.


2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kiran Singh ◽  
Parvesh Puri ◽  
Yogender Kumar ◽  
Chetan Sharma

This paper deals with the syntheses and structural features of some new diorganosilicon(IV) and diorganotin(IV) complexes having general formulae (CH3)2MCl(L1), (CH3)2MCl(L2), (CH3)2M(L1)2, and (CH3)2M(L2)2 with new Schiff bases (M = Si and Sn). The Schiff bases HL1 and HL2 have been derived from the condensation of 3-bromobenzaldehyde with 4-amino-3-ethyl-5-mercapto-1,2,4-triazole and 4-amino-5-mercapto-3-propyl-1,2,4-triazole, respectively. The compounds have been characterized by the elemental analyses, molar conductance, and spectral (UV, IR, 1H, 13C, 29Si, and 119Sn NMR) studies. The resulting complexes have been proposed to have trigonal bipyramidal and octahedral geometries. In vitro antimicrobial activities of the compounds have been carried out.


2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
C. Mallikarjunaswamy ◽  
D. G. Bhadregowda ◽  
L. Mallesha

Pyrimidine salts such as 2-methyl-5-nitro-phenyl-(4-pyridin-3-yl-pyrimidin-2-yl)-amine (1) and 4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-yl-amino)-phenyl-amine (2) with chloranilic and picric acids were synthesized, and theirin vitroantibacterial and antifungal activities were evaluated. The synthesized compounds were characterized by elemental analyses, UV-visible, FT-IR, and1H NMR spectral studies. Compound2aexhibited good inhibition towards antimicrobial activity compared to the other compounds.


2018 ◽  
Vol 2018 ◽  
pp. 1-12 ◽  
Author(s):  
K. Savithri ◽  
H. D. Revanasiddappa

Two novel oxidovanadium(IV) complexes with a new bidentate (O- and N-) imine-based ligand 2-((E)-(6-fluorobenzo[d]thiazol-2-ylimino)methyl)-6-methoxyphenol (HL) were synthesized under in situ experimental condition where VOSO4 acts as a kinetic template in the ratio 2 : 1 (L : M) and mixed ligand complex using 1,10-phenanthroline (phen) in 1 : 1 : 1 (L : M : phen) ratio. The synthesized compounds were structurally characterized by microanalysis, magnetic susceptibility, FTIR, electronic spectra, TG/DTA, ESR, and molar conductance studies. Based on the spectral studies, the complexes have the general composition [VO(L)2] (C1) and [VO(L)phen] (C2) in a square pyramid geometrical fashion. The synthesized compounds were primarily screened for their in vitro growth inhibiting activity against different strains of bacteria, namely, E. coli, B. subtilis, S. aureus, and P. aeruginosa by the disc diffusion method. Also, the antifungal activity was determined against C. albicans and A. niger by the Bateman poisoned technique. The in vitro antioxidant activity of all the compounds was determined by DPPH free radical-scavenging assay. Intercalative mode of DNA-binding properties of the oxidovanadium(IV) complexes with calf-thymus DNA (CT-DNA) was investigated using UV, fluorescence spectra, and viscosity measurements.


Author(s):  
Aseel Alsarahni ◽  
Zuhair Muhi Eldeen ◽  
Elham Al-kaissi ◽  
Ibrahim Al- Adham ◽  
Najah Al-muhtaseb

<p><strong>Objective: </strong>To design and synthesize amino acetylenic and thiocarbonate of 2-mercapto-1,3-benthiazoles as potential antimicrobial agents.</p><p><strong>Methods: </strong>A new series of 2-{[4-(t-amino-1-yl) but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole derivatives (AZ1-AZ6), and S-1,3-benzothiazol-2-yl-O-alkyl carbonothioate derivatives were synthesised, with the aim that the target compounds show new and potential antimicrobial activity. The elemental analysis was indicated by the EuroEA elemental analyzer, and biological characterization was via IR, <sup>1</sup>H-NMR, [13]C-NMR, DSC were determined with the aid of Bruker FT-IR and Varian 300 MHz spectrometer using DMSO-d<sub>6</sub> as a solvent.<em> </em><em>In vitro </em>antimicrobial activity, evaluation was done for the synthesised compounds, by agar diffusion method and broth dilution test. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined. <em></em></p><p><strong>Results: </strong>The IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, DSC and elemental analysis were consistent with the assigned structures. Compound of 2-{[4-(4-methylpiperazin-1-yl)but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole (AZ1), 2-{[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]sulfanyl}-1,3-benzothiazole (AZ2), 2-{[4-(piperidin-1-yl) but-2-yn-1-yl]sulfanyl}-1, 3-benzothiazole (AZ6), S-1,3-benzothiazol-2-yl-O-ethyl carbonothioate (AZ7), and S-1,3-benzothiazol-2-yl-O-(2-methylpropyl) carbonothioate (AZ9) showed the highest antimicrobial activity against <em>Pseudomonas aeruginosa </em>(<em>P. aeruginosa</em>), AZ-9 demonstrated the highest antifungal activity against <em>Candida albicans </em>(<em>C. albicans</em>), with MIC of 31.25 µg/ml.</p><p><strong>Conclusion: </strong>These promising results promoted our interest to investigate other structural analogues for their antimicrobial activity further.</p>


2012 ◽  
Vol 9 (3) ◽  
pp. 532-540 ◽  
Author(s):  
Baghdad Science Journal

Two Schiff base ligands L1 and L2 have been obtained by condensation of salicylaldehyde respectively with leucylalanine and glycylglycine then their complexes with Zn(II)were prepared and characterized by elemental analyses , conductivity measurement , IR and UV-Vis .The molar conductance measurement indicated that the Zn(II) complexes are 1:1 non-electrolytes. The IR data demonstrated that the tetradentate binding of the ligands L1 and L2 . The in vitro biological screening effect of the investigated compounds have been tested against the bacterial species Staphlococcus aureus, Escherichia coil , Klebsiella pneumaniae, Proteus vulgaris and Pseudomonas aeruginosa by the disc diffusion method . A comparative study of inhibition values of the Schiff base ligands and their complexes indicated that the complexes exhibit higher antimicrobial activity than the free ligands . Zinc ions are proven to be essential for the growth-inhibitor effect. The extent of inhibition appeared to be strongly dependent on the initial cell density and on the growth medium .


2009 ◽  
Vol 6 (3) ◽  
pp. 615-624 ◽  
Author(s):  
K. Siddappa ◽  
K. Mallikarjun ◽  
Tukaram Reddy ◽  
M. Mallikarjun ◽  
C. V. Reddy ◽  
...  

A new complexes of the type ML, MʹL and M″L [where M=Cu(II), Co(II), Ni(II) and Mn(II), Mʹ=Fe(III) and M″=Zn(II), Cd(II) and Hg(II) and L=N1-[(1E)-1-(2-hydroxyphenyl)ethylidene]-2-oxo-2H-chromene- 3-carbohydrazide (HL)] Schiff base have been synthesized and characterized by elemental analysis, magnetic susceptibility, molar conductance, IR,1H NMR, UV-Visible and ESR data. The studies indicate the HL acts as doubly monodentate bridge for metal ions and form mononuclear complexes. The complexes Ni(II), Co(II), Cu(II) Mn(II) and Fe(III) complexes are found to be octahedral, where as Zn(II), Cd(II) and Hg(II) complexes are four coordinated with tetrahedral geometry. The synthesized ligand and its metal complexes were screened for their antimicrobial activity.


1989 ◽  
Vol 9 (6) ◽  
pp. 2464-2476
Author(s):  
M Cockell ◽  
B J Stevenson ◽  
M Strubin ◽  
O Hagenbüchle ◽  
P K Wellauer

Footprint analysis of the 5'-flanking regions of the alpha-amylase 2, elastase 2, and trypsina genes, which are expressed in the acinar pancreas, showed multiple sites of protein-DNA interaction for each gene. Competition experiments demonstrated that a region from each 5'-flanking region interacted with the same cell-specific DNA-binding activity. We show by in vitro binding assays that this DNA-binding activity also recognizes a sequence within the 5'-flanking regions of elastase 1, chymotrypsinogen B, carboxypeptidase A, and trypsind genes. Methylation interference and protection studies showed that the DNA-binding activity recognized a bipartite motif, the subelements of which were separated by integral helical turns of DNA. The alpha-amylase 2 cognate sequence was found to enhance in vivo transcription of its own promoter in a cell-specific manner, which identified the DNA-binding activity as a transcription factor (PTF 1). The observation that PTF 1 bound to DNA sequences that have been defined as transcriptional enhancers by others suggests that this factor is involved in the coordinate expression of genes transcribed in the acinar pancreas.


2019 ◽  
Vol 2019 ◽  
pp. 1-14 ◽  
Author(s):  
Dorian Polo-Cerón

This paper reports the synthesis and detailed characterisation of copper(II) and nickel(II) complexes with tridentate thiosemicarbazone ligands H2L1 and H2L2 derived from 2-acetylpyrazine. The ligands and their metal complexes were characterised by different physicochemical techniques, including elemental and thermogravimetric analysis; UV-Vis, IR, 1H-NMR, and 13C-NMR spectroscopy; molar conductance measurements; and mass spectrometry. The crystal structure of the H2L1 ligand was determined by single crystal X-ray diffraction studies. The spectral data showed that the thiosemicarbazone behaves as an NNS tridentate ligand through the nitrogen atoms of the azomethine group and pyrazine ring and the sulphur atom of the thioamide group. Elemental and thermal analyses indicated that the obtained metal complexes had a 1 : 1 stoichiometry (metal-ligand). The interactions between these complexes and calf thymus DNA (CT-DNA) were studied by electronic absorption and viscosity measurements. The activities of these compounds against oxidative DNA cleavage were examined by agarose gel electrophoresis. Cu(II) and Ni(II) complexes can wind DNA strands through groove interactions and promote strand breakage of the plasmid pmCherry under oxidative stress conditions. Moreover, all the complexes could interact more strongly with DNA than could with the free ligands. Finally, the antibacterial activities of the ligands and their complexes were determined by in vitro tests against Gram-positive bacterial strains (S. aureus ATCC 25923, L. monocytogenes ATCC 19115, and B. cereus ATCC 10876) and Gram-negative bacterial strains (E. coli ATCC 25922, S. typhimurium ATCC 14028, and K. pneumoniae ATCC BAA-2146) using the broth microdilution method. The metal complexes showed greater antimicrobial activities than the precursor ligands against some of the microorganisms.


2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Har Lal Singh ◽  
Jangbhadur Singh

New series of organotin(IV) complexes and Schiff bases derived from amino acids have been designed and synthesized from condensation of1H-indole-2,3-dione, 5-chloro-1H-indole-2,3-dione, andα-amino acids (phenylalanine, isoleucine, and glycine). All compounds are characterized by elemental analyses, molar conductance measurements, and molecular weight determinations. Bonding of these complexes is discussed in terms of their UV-visible, infrared, and nuclear magnetic resonance (1H,13C, and119Sn NMR) spectral studies. The results suggest that Schiff bases behave as monobasic bidentate ligands and coordinate with dibutyltin(IV) in octahedral geometry according to the general formula [Bu2Sn(L)2]. Elemental analyses and NMR spectral data of the ligands with their dibutyltin(IV) complexes agree with their proposed distorted octahedral structures. Few representative compounds are tested for their in vitro antibacterial activity against Gram-positive (B. cereus,Staphylococcusspp.) and Gram-negative (E. coli,Klebsiellaspp.) bacteria. The results show that the dibutyltin complexes are more reactive with respect to their corresponding Schiff base ligands.


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