scholarly journals Synthesis and Characterization of Cobalt(III) and Copper(II) Complexes of 2-((E)-(6-Fluorobenzo[d]thiazol-2-ylimino) methyl)-4-chlorophenol: DNA Binding and Nuclease Studies—SOD and Antimicrobial Activities

2018 ◽  
Vol 2018 ◽  
pp. 1-15 ◽  
Author(s):  
K. Savithri ◽  
B. C. Vasantha Kumar ◽  
H. K. Vivek ◽  
H. D. Revanasiddappa
Keyword(s):  
Metal Complexes ◽  
Antimicrobial Activities ◽  
Spectroscopic Studies ◽  
Docking Studies ◽  
Bacterial Strains ◽  
Spectral Techniques ◽  
Light Reduction ◽  
Drug Candidates ◽  
Ft Ir

A bidentate (N- and O-) imine-based ligand (L1) and its metal complexes of types [CuII(L1)2] (C1), [CuII(L1)(Phen)] (C2), [CoIII(L1)2] (C3), and [CoIII(L1)(Phen)] (C4) (L1 = 2-((E)-(6-fluorobenzo[d]thiazol-2-ylimino)methyl)-4-chlorophenol and phen = 1,10-phenanthroline) were synthesized as potential chemotherapeutic drug candidates. The prepared complexes were structurally characterized by spectral techniques (NMR, FT-IR, LC-MS, EPR, and electronic absorption), thermogravimetric analysis (TGA/DTA), magnetic moment, and CHNO elemental analysis. Spectroscopic studies suggested the distorted octahedral structure for all complexes. In vitro bioassay studies include binding and nuclease activities of the ligand and its complexes with target calf thymus- (CT-) DNA were carried out by employing UV-Vis, fluorescence spectroscopy, viscosity, and gel electrophoresis techniques. The extent of binding propensity was determined quantitatively by Kb and Ksv values which revealed a higher binding affinity for C2 and C4 as compared to C1 and C3. In addition, the scavenging superoxide anion free radical (O∙-2) activity of metal complexes was determined by nitroblue tetrazolium (NBT) light reduction assay. Molecular docking studies with DNA and SOD enzyme were also carried out on these compounds. The antimicrobial study has shown that all the compounds are potential antibacterial agents against Gram-negative bacterial strains and better antifungal agents with respect to standard drugs used.

scholarly journals Fungal Biotransformation of Cyclademol and Antimicrobial Activities of Its Metabolites

2017 ◽  
Vol 12 (10) ◽  
pp. 1934578X1701201
Author(s):  
Ismail Kiran ◽  
Özge Özşena ◽  
K Hüsnü Can Başer ◽  
Fatih Demirci
Keyword(s):  
Aspergillus Niger ◽  
Neurospora Crassa ◽  
Antimicrobial Activities ◽  
Spectroscopic Studies ◽  
Bacterial Strains ◽  
Fungal Strains ◽  
Agar Dilution ◽  
Ft Ir ◽  
First Time

Cyclademol (1) was converted for the first time to 1-(4-hydroxy-3,3-dimethylcyclohexyl) ethanone (2) and 4-(1-hydroxyethyl)-2,2-dimethylcyclohexanol (3) with 31.2 and 15.1% yields by Aspergillus niger and Neurospora crassa, respectively. The resulting metabolite structures were established by FT-IR, MS and NMR spectroscopic studies, respectively. In addition, the in vitro antimicrobial activities of the substrates and metabolites were evaluated comparatively both by using agar dilution and microdilution methods. The minimum inhibitory concentrations (MIC) of the tested compounds against a panel of pathogenic bacterial strains ranged from 1000 - 4000 μg/mL, whereas the MIC values against fungal strains were between 500 −1000 μg/mL.

scholarly journals SYNTHESIS, SPECTRAL CHARACTERIZATION AND ANTIMICROBIAL ACTIVITIES OF BIS(CYCLOPENTADIENYL)TITANIUM(IV) COMPLEXES WITH SCHIFF BASES DERIVED FROM5-(SUBSTITUTED ARYL)-2-HYDRAZINO-1, 3, 4-OXADIAZOLE AND INDOLINE-2, 3-DIONE

2021 ◽  
Vol 9 (09) ◽  
pp. 900-909
Author(s):  
Anupama Srivastava ◽  
◽  
Shilpi Srivastava ◽  
Om. P. Pandey ◽  
Soumitra K. Sengupta ◽  
...  
Keyword(s):  
Schiff Bases ◽  
Electrical Conductance ◽  
Antimicrobial Effect ◽  
Antimicrobial Activities ◽  
Molar Conductance ◽  
Bacterial Strains ◽  
Monoclinic Crystal ◽  
Spectral Techniques ◽  
Concentration Method

Titanium(IV) complexes of type[(η5-C5H5)2TiCl(L)] have been synthesized by the reactions of bis(cyclopentadienyl)titanium(IV)dichloride with Schiff bases (LH) derived by the condensation of 5-(substituted aryl)-2-hydrazino-1,3,4-oxadiazole and indoline-2,3-dione in tetrahydrofuranin the presence oftriethylamine. All these complexes are soluble in PhNO2, DMF and DMSO.The complexes were characterized by elemental analyses, electrical conductance, magnetic susceptibility, UV-Vis, IR, 1H NMR, 13C NMR, XRD and SEM spectral techniques. Low molar conductance values indicate that they are non-electrolytes. The spectral data indicate5-coordinate geometry for the complexes.XRD pattern indicate that the complexes have monoclinic crystal system and particle sizes were found 49.36 nm (nano-size). In vitro antifungal activity of synthesized compounds was evaluated against fungi Aspergillusniger, Aspergillusflavus,ColletotrichumfalcatumandIn vitro antibacterial activity was determined by screening the compounds against gram negative (P. aeruginosa, S.typhi) and gram positive (S. aureus and B.subtilis) bacterial strains using minimum inhibition concentration method (MIC) by serial dilution technique. The titanocene(IV) complexes have higher antimicrobial effect than the parent Schiff bases.

scholarly journals Cu(II) and Ni(II) Complexes with New Tridentate NNS Thiosemicarbazones: Synthesis, Characterisation, DNA Interaction, and Antibacterial Activity

2019 ◽  
Vol 2019 ◽  
pp. 1-14 ◽  
Author(s):  
Dorian Polo-Cerón
Keyword(s):  
Metal Complexes ◽  
Dna Cleavage ◽  
Thermal Analyses ◽  
Dna Interaction ◽  
Antimicrobial Activities ◽  
Tridentate Ligand ◽  
Bacterial Strains ◽  
Azomethine Group ◽  
Broth Microdilution Method

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.

scholarly journals MCF-7 Human Breast Adenocarcinoma Anticancer and Antimicrobial, in silico Docking and ADME Prediction Studies of Furan Moiety Containing Substituted 2-Aminopyrimidine Derivatives

2021 ◽  
Vol 33 (7) ◽  
pp. 1504-1512
Author(s):  
Manju Mathew ◽  
Muthuvel Ramanathan Ezhilarasi
Keyword(s):  
In Silico ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
Breast Adenocarcinoma ◽  
Bacterial Strains ◽  
In Silico Docking ◽  
In Silico Studies ◽  
Furan Moiety ◽  
Different Strains

A series of 4(5-(4-chlorophenyl)furan-2-yl)-6-phenylpyrimidin-2-amine derivatives (5a-h) were synthesized from 2-(4-chlorophenyl)-5-styrylfuran (3a-h) with guanidine nitrate in absolute ethanol under conventional method and evaluated for their in vitro anticancer, antimicrobial activities and in silico studies. The chemical structure of the furan moiety containing substituted amino pyrimidine derivatives (5a-h) were elucidated from spectroscopic analysis like infrared, 1H & 13C NMR spectral data and CHN analysis. in silico docking studies were predicted for the synthesized compounds (5a-h) using bacterial protein 1UAG and in silico ADME predictions were also carried for the synthesized compounds (5a-h). The in vitro anticancer study was carried the compound 5b by MMT assay. Compound 5b shows the LC50 value of 120.15 ± 0.003 μg/mL. in vitro Antimicrobial activities were screened for the compounds (5a-h) using different strains. Compound 5h has electron withdrawing group in benzene ring substituted in the para position showed good antimicrobial activity against all the bacterial strains and fungal strains. in silico studies, compound 5h shows excellent docking score (-9.7 kcal/mol) compared with ciprofloxacin (-7.8 kcal/mol).

scholarly journals Antitumor and Antimicrobial Potential of Manganese(II), Nickel(II) and Copper(II) Complexes of 4-Methoxy Benzohydrazide Derived Schiff Base Ligand

2021 ◽  
Vol 11 (1) ◽  
pp. 3249-3260
Keyword(s):  
Schiff Base ◽  
Metal Complexes ◽  
Schiff Base Ligand ◽  
Antimicrobial Activities ◽  
Molar Ratio ◽  
Gram Positive Bacteria ◽  
Ft Ir ◽  
Dose Dependent

Herein, we describe the synthesis and characterization of a Schiff base ligand (E)-N'-(2-hydroxybenzylidene)-4-methoxybenzohydrazide (HBMB) and its Mn(II), Ni(II), and Cu(II) metal complexes (C1-C3) respectively. The ligand HBMB was synthesized by reacting condensation of salicylaldehyde and 4-methoxy benzohydrazide in a 1:1 molar ratio. The structure of HBMB and its metal complexes (C1-C3) were evaluated by using UV-Vis, FT-IR, 1H-NMR, mass spectroscopy as well as on the basis of elemental analysis, conductivity measurements, and thermogravimetric techniques (TGA). The synthesized molecules' tumoricidal properties were performed against human breast cancer (MCF-7) and colon cancer (HT 29) cell lines. The biological results indicated that the ligand, HBMB, and metal complexes possess dose-dependent selective cytotoxicity against the tested carcinoma cells. The synthesized compounds were further evaluated for their in vitro antimicrobial activities against Gram-positive bacteria (Staphylococcus aureus), Gram-negative bacteria (Escherichia coli), and fungal strains (Aspergillus niger).

scholarly journals Synthesis, Molecular Docking and Antimicrobial Activities of 5-(4-substituted-benzyl)-2-(furan/thiophen-2-ylmethylene hydrazono)thiazolidin-4-ones

2021 ◽  
Vol 11 (4) ◽  
pp. 12434-12446
Keyword(s):  
Escherichia Coli ◽  
Molecular Docking ◽  
1H Nmr Spectroscopy ◽  
Antimicrobial Properties ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
Binding Affinities ◽  
Bacterial Strains ◽  
Effective Synthesis

In our present work, we reported an effective synthesis, molecular docking, and antimicrobial properties of novel 5-(4-substituted-benzyl)-2-(furan/thiophen-2-ylmethylene hydrazono) thiazolidin-4-ones (6a-g) and (7a-i). The structures of the synthesized compounds (6a-g) and (7a-i) were elucidated by 1H-NMR spectroscopy. The molecular docking studies were performed for all the synthesized compounds against GlcN-6P using AutoDock-tools-1.5.6 and recorded the extent of H-bonding and binding affinities. The preselected compounds via molecular docking were further tested for in vitro antimicrobial activity against five bacterial strains (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus) and two fungal strains (Candida albicans and Cryptococcus neoformans). The antimicrobial findings exhibited that the compounds possessed significant antimicrobial potential.

scholarly journals Design, Sustainable Synthesis, Characterization, Antimicrobial Evaluation and in silico ADMET Prediction of New Functionalized Imidazolium Based Ionic Liquids

2020 ◽  
Vol 32 (8) ◽  
pp. 1972-1980
Author(s):  
Anas R. Al Johani ◽  
Saud M. Almutairi ◽  
Wael S. El-Sayed ◽  
Pramod K. Sahu ◽  
Praveen K. Sahu ◽  
...  
Keyword(s):  
Ionic Liquids ◽  
In Silico ◽  
Phenyl Group ◽  
Antimicrobial Activities ◽  
Spectral Techniques ◽  
In Silico Admet ◽  
Antimicrobial Evaluation ◽  
Ft Ir

A series of sixteen new ionic liquids (ILs) bearing imidazolium moiety were designed and synthesized under sustainable and green conditions which were confirmed by analytical and spectral techniques using 1H- & 13C-NMR, FT-IR, mass and elemental analysis. A panel of clinically isolated strains was used for in vitro inhibitory antimicrobial activities screening of synthesized ionic liquids. The results of antimicrobial assay showed that some of synthesized ionic liquids showed moderate to good activity. Among these ILs, ionic liquids 3, 4 and 5 (bearing alkyl chain with a phenyl group) significantly inhibited cell growth of strains. In this regard, these ionic liquids considered as promising antibacterial agents when compared with standard antibiotics. By encouraging in vitro antimicrobial screening, in silico ADMET evaluation has been performed and found excellent pharmacokinetic, bioavailability and toxicity profiles. Synthesized ionic liquids has found to be safe and non-toxic according to calculated in vivo computed LD50 values (2.49-2.80 mg/kg) for rat acute toxicity.

scholarly journals Synthesis, Characterization and in Vitro Antimicrobial Studies of Ternary Mn(II) Complexes with Isatinphenylhydrazone, Glycine and 8-hydroxyquinoline

2021 ◽  
Vol 37 (5) ◽  
pp. 1146-1151
Author(s):  
Suman Kumari ◽  
Shobhana Sharma ◽  
Seema Seema ◽  
Poonam Yadav ◽  
Mamta Ranka
Keyword(s):  
Complex I ◽  
Research Work ◽  
Analytical Techniques ◽  
Antimicrobial Activities ◽  
Molar Conductance ◽  
Bacterial Strains ◽  
Spectral Techniques ◽  
Molar Ratios ◽  
Antimicrobial Studies

In our present research work, we have synthesized two ternary metal complexes of Mn(II), complex-I as [Mn(L)(Gly)(Cl)(H2O)] and complex-II as [Mn(L)(Q)(Cl)(H2O)]; where L is Isatinphenylhydrazone (IPH) as primary ligand, whereas glycine (Gly) and 8-hydroxyquinoline (HQ) as secondary ligand in complex-I and II respectively, in 1:1:1 (M : L : Gly or M : L : Q) molar ratios. Above synthesized complexes are employed for characterization using various analytical techniques including elemental analysis, melting point determination, magnetic moment measurements, molar conductance measurements, and spectral techniques (FTIR, UV, 1H NMR) etc. Further, their antimicrobial activities were evaluated against selected bacterial strains i.e., B. subtilis, S. aureus (Gram positive) and P. aeruginosa, E. coli (Gram negative) and fungal strains (T. reesei, A. niger, C. albicans) and found significantly active.

scholarly journals Studies on the Spectral, Anti-Bacterial and Anti-Fungal Activities of 1-((Dicyclohexylamino) (Phenyl) Methyl) Pyrrolidine-2, 5-Dione and Few of its Metal Complexes

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 3124-3136
Author(s):  
Rajeswari S ◽  
Harindran Suhana ◽  
Kalaivizhi R
Keyword(s):  
Metal Complexes ◽  
Mannich Base ◽  
Micrococcus Luteus ◽  
Free Ligand ◽  
Antimicrobial Activities ◽  
Spectral Studies ◽  
Aspergillus Fumigates ◽  
Ft Ir ◽  
Anti Fungal

1-((dicyclohexylamino)(phenyl)methyl) pyrrolidine-2,5-dione (SDB) has been synthesized as a result of succinimide, benzaldehyde and dicyclohexylamine Mannich base condensation and its CoII, NiII and CuII complexes were prepared. The structure of the Mannich Base ligand (SDB) was elucidated on the basis of FT-IR, 1H NMR, 13C NMR and Mass spectral studies. The monomeric and non-electrolytic nature of the metal complexes is evidenced by their magnetic susceptibility and low conductance data studies. Spectral tests, mainly FT-IR studies as well as elemental analysis, were carried out to verify the structures of the newly synthesized compounds. All the metal complexes possess a six-coordinate geometry. The synthesized ligand and its metal complexes have been tested against Gram-positive strains (Staphylococcus aureus and Micrococcus luteus), Gram-negative strains (Escherichia coli and Pseudomonas aeruginosa) and fungal strains (Aspergillus niger and Aspergillus fumigates) for their in vitro anti-bacterial and anti-fungal activities. Preliminary antimicrobial studies of the ligand and their metal complexes have also been carried out in order to understand the toxic effect of ligands and metal complexes against the selective microbes. The results showed that the metal chelates of the ligands showed higher antimicrobial activities than the free ligand SDB and CoII  complexes possess higher activity than the other metal complexes. 

scholarly journals Synthesis and Biological Evaluation of m-PEG Attached Acridinedione Derivatives as Antimicrobial, Antioxidant and Anticancer Agents

2021 ◽  
Vol 33 (7) ◽  
pp. 1603-1610
Author(s):  
Tathagata Dey ◽  
Indira Viswambaran Asharani
Keyword(s):  
Anticancer Agents ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Anticancer Activities ◽  
Gram Positive ◽  
Spectral Techniques ◽  
Drug Candidates ◽  
Anticancer Properties ◽  
Gram Negative Organisms

Among heterocycles, a wide variety of nitrogen heterocycles have been exploited to develop pharmaceutically important molecules. Particularly, acridines are clinically used potential drug candidates showing various pharmacological activities. Some of the novel m-PEG attached acridinediones 4(a-j) were synthesized with the readily available starting materials such as dimedone, glycine and aldehydes. Structures of the synthesized compounds were characterized by spectral techniques. The synthesized compounds (4a-j) were evaluated for in vitro antimicrobial, antioxidant and anticancer activities. Compounds 4d, 4e and 4g were found to produce potent antimicrobial activities against Gram-positive and Gram-negative organisms while 4c active against only Gram-positive organisms when compared with the standard, ciprofloxacin. On the other side, 4d and 4i produced potent antioxidant activity and 4a, 4d and 4g exhibited comparable anticancer properties.

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