scholarly journals Synthesis, Characterization, in silico and in vitro Studies of Transition Metal Complexes with Biologically Active Ligand as Antigout Agent Colchicine

2020 ◽  
pp. 107-114
Author(s):  
Vaishali Gaikwad ◽  
Vaibhav Sabale ◽  
Bhimrao Khade
Keyword(s):  
Antimicrobial Activity ◽  
Binding Energy ◽  
Transition Metals ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Biologically Active ◽  
Polymerization Inhibitor ◽  
Tubulin Polymerization Inhibitor ◽  
Parent Ligand

Colchicine is essentially useful in the treatment of gout. In the present work Colchicine Complexes has been prepared with transition metals viz; Copper(II) [Cu(II)], Zinc (II) [Zn(II)], Cobalt (II) [Co(II)], Nickel (II) [Ni(II)] and those checked for molecular docking, it has been observed that Zn(II) and Ni(II) complex has revealed good binding energy than the parent ligand, the increased binding energy of colchicine metal complexes  indicates that, the tubulin polymerization inhibitor tendency is enhanced, consequently antigout property is also increased. As transition metals have antimicrobial activity in themselves, complexes are also characterized for the antimicrobial activity which is enhanced for Cu(II) and Co(II) metals.

scholarly journals SYNTHESIS, CHARACTERIZATION, IN VITRO ANTIMICROBIAL, ANTHELMINTIC AND DOCKING STUDIES OF NEW 2-[(E)-{[4-(1H-1,2,4-TRIAZOL-1 YLMETHYL)PHENYL]IMINO} METHYL]PHENOL, AND THEIR COMPLEXES WITH 3D METAL IONS

2016 ◽  
Vol 8 (9) ◽  
pp. 134
Author(s):  
Jithendra Kumara K.s. ◽  
Krishnamurthy G. ◽  
Sunil Kumar N.
Keyword(s):  
Antimicrobial Activity ◽  
Schiff Base ◽  
Transition Metal ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Research Work ◽  
Anthelmintic Activity ◽  
Triazole Ring ◽  
Diffusion Method

<p><strong>Objective: </strong>The main objectives of this research work is the synthesis and characterization of biologically potential triazole ring containing the Schiff base legend and their transition metal complexes, followed by screenings of their antimicrobial and anthelmintic activity the results of antimicrobial activity were compared with docking scores.</p><p><strong>Methods: </strong>The<strong> </strong>coordination complexes of Co(II), Cu(II), Fe(III) and Zn(II) with Schiff base derived ligand 4-(1<em>H</em>-1,2,4-triazol-1-ylmethyl) aniline and substituted aldehydes have been synthesized. The complexes are characterized by elemental analysis, conductivity measurements, electronic, IR, and <sup>1</sup>H NMR spectral data. The synthesized compounds were also screened <em>In vitro</em> antimicrobial activity was carried out according to diffusion method by using agar and potato dextrose agar at 100, 500 and 700 mg/ml concentrations in DMF.<strong> </strong>HEX 8.0<strong> </strong>programmers were used to perform the docking experiments on <em>nucleotide </em>of <em>S. typhi </em><em>at</em> as ligand [PDB: 3B6O].</p><p><strong>Results: </strong>Schiff base ligand and their transition metal complexes were studied for antimicrobial activity as well as docking. The results of both studies concluded that 4a, 4c and 4d compounds are more active in minimum inhibition concentration (30μg/ml) against <em>Staphylococcus aureus</em> (<em>S. aureus), Salmonella typhi (S. typlei)</em> bacteria and <em>Penicillium chrysogenum</em> (<em>P. Crysogenum) </em>fungi. The compounds showed highest docking score (-257.47,-275.61 and-280.17 respectively) with the secondary structure of the alpha-amylase with a nucleotide from <em>s. typhi</em> in the solid model. In the study of anthelmintic activity among these three compounds, 4d compound exhibits more activity compared with the standard.</p><strong>Conclusion: </strong>The compounds 4a, 4c and 4d were found to be more promising pharmacological activity this observation may promote a further development of this triazole group of compounds which may lead to better pharmacological profile than standard drugs. <p> </p>

Synthesis, Characterization and in vitro Biological Evaluation of a New Schiff Base Derived from Drug and its Complexes with Transition Metal Ions

2018 ◽  
Vol 69 (7) ◽  
pp. 1678-1681
Author(s):  
Amina Mumtaz ◽  
Tariq Mahmud ◽  
M. R. J. Elsegood ◽  
G. W. Weaver
Keyword(s):  
Schiff Base ◽  
Transition Metal ◽  
Metal Ions ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Free Ligand ◽  
Transition Metal Ions ◽  
Biological Evaluation ◽  
Pyridoxal Hydrochloride

New series of copper (II), cobalt (II), zinc (II), nickel (II), manganese (II), iron (II) complexes of a novel Schiff base were prepared by the condensation of sulphadizine and pyridoxal hydrochloride. The ligand and metal complexes were characterized by utilizing different instrumental procedures like microanalysis, thermogravimetric examination and spectroscopy. The integrated ligand and transition metal complexes were screened against various bacteria and fungus. The studies demonstrated the enhanced activity of metal complexes against reported microbes when compared with free ligand.

Endo- and exohedral chloro-fulleride as η5 ligands: A DFT study on the first-row transition metal complexes

2021 ◽  
Author(s):  
Sebastian Anila ◽  
Cherumuttathu Hariharan Suresh
Keyword(s):  
Transition Metal ◽  
Transition Metals ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Dft Study ◽  
C60 Fullerene ◽  
Ring Fusion ◽  
Coordination Modes

C60 fullerene coordinates to transition metals in η2-fashion through its C-C bond at [6,6] ring fusion whereas other coordination modes η3, η4, η5 and η6 are rarely observed. The coordination...

Transition metal complexes with monodeprotonated isoorotic and 2-thioisoorotic acids: Crystal structure, spectral and magnetic study, and antimicrobial activity

1993 ◽  
Vol 51 (3) ◽  
pp. 613-632 ◽  
Author(s):  
F. Hueso-Ureña ◽  
M.N. Moreno-Carretero ◽  
M.A. Romero-Molina ◽  
J.M. Salas-Peregrin ◽  
M.P. Sanchez-Sanchez ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Antimicrobial Activity ◽  
Transition Metal ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Magnetic Study

scholarly journals The Search for Biologically Active Compounds in the Series of N-ethoxyethylpiperidine Derivatives

2019 ◽  
Vol 21 (2) ◽  
pp. 125
Author(s):  
U.B. Issayeva ◽  
G.S. Akhmetova ◽  
U.M. Datkhayev ◽  
M.T. Omyrzakov ◽  
K.D. Praliyev ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Biologically Active ◽  
Hydroxyl Group ◽  
Diffusion Method ◽  
Acylation Reaction ◽  
Gram Positive Bacteria ◽  
Cyclopropanecarboxylic Acid ◽  
Yeast Fungus ◽  
Acid Esters

With the aim to introduce fragment of cyclopropane and fragments of p-, m-, o-fluorophenyls into the structures of N-ethoxyethylpiperidines, acylation of oxime and phenylacetylenic alcohol of 1-(2-ethoxyethyl)-4-ketopiperidine by cyclopropanecarbonylchloride was carried out; on the basis of 1-(2-ethoxyethyl)-4-ethynyl-4-hydroxypiperidine (cascaine alcohol), acylation by 4-fluoro-, 3-fluoro-, 2-fluorobenzoylchlorides was carried out with formation of the corresponding piperidine containing hydrochlorides of cyclopropanecarboxylic acid esters and para-, meta-, ortho-fluorobenzoic esters. Acylation reaction on the hydroxyl group of compounds is carried out in absolute dioxane, the acylating agents are cyclopropanecarbonylchloride, p-, m-, o-fluorobenzoyl chlorides taken in excess. The obtained esters of cyclopropanecarboxylic and para-, meta-, ortho-fluorobenzoic acids are crystalline substances with a clear melting point, well soluble in water, ethanol, acetone. P-fluorobenzoates are obtained with better yields, m-fluorobenzoates occupy an intermediate position, and o-fluorobenzoates are formed with the lowest yields. The best yields of fluorobenzoates are obtained using dioxane as a solvent. Para-, meta-, ortho-fluorobenzoic esters of 1-(2-ethoxyethyl)-4-ethynyl-4-hydroxypiperidine coded A-4 – A-6 were studied for the presence of antimicrobial activity, the actions of these preparations were evaluated in vitro in relation to strains of gram-positive bacteria Staphylococcus aureus, Bacillus subtilis, gram-negative strains of Escheriсhia coli, Pseudomonas aeruginosa and to yeast fungus Сandida albicans by the diffusion method into agar (holes). Introduction of fluorine atom into the structure of cascaine lead to manifestation of antimicrobial activity.

scholarly journals A new group of compounds derived from 4-, 5-, 6- and 7-aminoindoles with antimicrobial activity

2018 ◽  
Vol 4 (3) ◽  
pp. 27-36 ◽  
Author(s):  
Irina Stepanenko ◽  
Semen Yamashkin ◽  
Yuliya Kostina ◽  
Alyona Batarsheva ◽  
Mikhail Mironov
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antibiotic Resistance ◽  
Biologically Active ◽  
Diffusion Method ◽  
Significant Activity ◽  
Clinical Strains ◽  
Causative Agents ◽  
New Compounds

Introduction. The problem of antibiotic resistance of microorganisms is becoming more urgent in the twenty-first century. Microorganisms possess an evolutionary adaptive capacity. Non-adherence to the basic principles of rational antibiotic therapy leads to menacing consequences. More and more pathogenic microbes are becoming resistant to two or more antibiotics. The search for new compounds with antimicrobial activity is one of the principles for overcoming the antibiotic resistance of microorganisms. Materials and methods. Eighteen test-strains of microorganisms and more than 2000 clinical strains of microorganisms, representating the families Micrococcaceae, Streptococcaceae, Enterobacteriaceae, Moraxellaceae, Pseudomonadaceae, Sphingomonadaceae, Xanthomonadaceae were studied for sensitivity to the compounds derived from 4-, 5-, 6- and 7-aminoindoles. A method of serial dilutions to determine the minimal inhibitory concentration (MIC) of the compounds under study was used in the study, as well as a disc diffusion method. Results and discussion. Sensitivity of the test-strains and of clinical strains of microorganisms to the resulting compounds was studied. The compounds based on substituted 4-, 5-, 6-, 7-aminoindoles showed different activity against the test strains and experimental strains of microorganisms in vitro. It was found that the marked antibacterial activity was exhibited by the compounds containing a trifluoromethyl group. The most significant activity was noted in amides and pyrroloquinolones based on 4-aminoindole, 6-aminoindole and 7-aminoindole.The most effective compounds with laboratory codes 5D, 7D, 39D, S3, HD, 4D showed a pronounced antibacterial activity. Conclusion. Antimicrobial activity of the substituted amides and pyrroloquinolines on the basis of 4-, 5-, 6-, 7-aminoindoles was etermined in our study, as well as the spectra of their action against Gram-positive and Gram-negative microorganisms, which are causative agents of non-specific and certain specific human infectious diseases. Moreover, we evaluated the synthetic potentials of the substituted 4-, 5-, 6-, 7-aminoindoles as the starting compounds for synthesizing a series of indolylamides and pyrroloquinolines. Also, the prospects for targeted synthesis of biologically active compounds based on indole-type aromatic amines were determined.

scholarly journals Synthesis and Modification of Some New Transition Metal Complexes of Poly (vinyl chloride)

2017 ◽  
Vol 14 (1) ◽  
pp. 202-207
Author(s):  
Baghdad Science Journal
Keyword(s):  
Transition Metal ◽  
Transition Metals ◽  
Metal Complexes ◽  
Ftir Spectroscopy ◽  
Vinyl Chloride ◽  
Transition Metal Complexes ◽  
Visible Spectroscopy ◽  
Poly Vinyl Chloride

Theligand4-[5-(2-hydoxy-phenyl)- [1,3,4- thiadiazole-2- ylimino methyl]-1,5-dimethyl -2-phenyl-1,2-dihydro-pyrazol-3-one [HL1] is prepared and characterized. It is reacted with poly(vinyl chloride) (PVC) in THF to form the PVC-L compounds ,PVC-L interacted with ions of transition metals to form PVC-L-MII complexes .All prepared compounds are characterized by FTIR spectroscopy, u.v-visible spectroscopy, C.H.N.S. analysis and some of them by 1HNMR

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