Synthesis, Design and Biological Evaluation of Antibacterial activity of novel mixed Metal Complexes derived from Benzoimidazolphenylethanamine and 6-Amino-N,N-dimethyluracil

2020 ◽  
Vol 17 ◽  
Author(s):  
Fahad M. Alminderej
Keyword(s):  
Metal Complexes ◽  
Micrococcus Luteus ◽  
Condensation Reaction ◽  
Antibacterial Activities ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Gram Positive Bacteria ◽  
Synthesis Design ◽  
Hybrid Complexes

: Benzoimidazolphenylethanamine (BPE) was synthesized through the condensation reaction of 1,2-phenyldiamine and L-phenylalanine. The new complexes were prepared from the reaction of 6-amino-N,N-dimethyluracil (ADU), benzoimidazolphenylethanamine and Cadmium (II), Tin (II), Copper (II) and Nickel (II) metal respectively. All new hybrid complexes were fully characterized by spectroscopic data of FTIR, UV-Visible electronic absorption, thermal analysis, X-ray powder diffraction studies and mass spectroscopy. Spectra analyses of the hybrid metal complexes showed the tetrahedral coordination of the ligands to the metal ions via the nitrogen atoms. The in vitro antibacterial activities of the hybrid complexes were assayed against four bacterial isolates namely, Micrococcus luteus, Staphylococcus aureus as gram positive bacteria, Pseudomonas aeruginosa and Escherichia coli as gram negative bacteria using agar well diffusion method. Most of the tested isolates were sensitive to most metal hybrid complexes. The drug likeness and bioactivity properties were calculated using Molinspiration Cheminformatics software.

scholarly journals Novel Mixed Complexes Derived from Benzoimidazolphenylethanamine and 4-(Benzoimidazol-2-yl)aniline: Synthesis, Characterization, Antibacterial Evaluation and Theoretical Prediction of Toxicity

2020 ◽  
Vol 32 (6) ◽  
pp. 1266-1272
Author(s):  
Lotfi M. Aroua
Keyword(s):  
Metal Complexes ◽  
Micrococcus Luteus ◽  
Condensation Reaction ◽  
Antibacterial Activities ◽  
Molar Ratio ◽  
Monoclinic System ◽  
Spectra Analysis ◽  
Mixed Metal Complexes ◽  
Uv Visible

Benzoimidazolphenylethanamine (BPE) has been synthesized using condensation reaction from o-phenyldiamine and L-phenylalanine. Some metal complexes have been synthesized from 4-(benzoimidazol-2-yl)aniline, benzoimidazolylphenylethanamine and cadmium(II), tin(II), copper(II) and nickel(II) metal in a molar ratio (1:1:1). All new metal complexes were characterized by spectroscopic data of FTIR, UV-visible electronic absorption, X-ray powder diffraction and thermal analysis. Spectra analysis of the mixed metal complexes showed the coordination of ligands to the metal ions via nitrogen atoms. The XRD powder showed that metal complexes have a monoclinic system. The preliminary tested in vitro antibacterial activities of Sn(II) complex was assayed against four bacterial isolates namely Micrococcus luteus, Staphylococcus aureus as Gram-positive, Pseudomonas aerugmosa and Escherichia coli.

scholarly journals Synthesis, Characterization and Biological Evaluation of Fe(III) and Cu(II) Complexes with 2,4-Dinitrophenyl hydrazine and Thiocyanate Ions

2019 ◽  
Vol 31 (4) ◽  
pp. 780-784
Author(s):  
P. Manimaran ◽  
S. Balasubramaniyan
Keyword(s):  
Antioxidant Activity ◽  
Metal Complexes ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Free Ligand ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Spectral Studies

The metal complexes of Fe(III) and Cu(II) were prepared by using 2,4-dinitrophenyl hydrazine (DNPH) and thiocyanate (SCN) with stirrer refluxed for about 6 h. The prepared Fe(III) and Cu(II) complexes were characterized by elemental analysis, molar conductance, magnetic susceptibility and electronic spectrum, FT-IR spectral studies. The result suggested the octahedral geometry for Fe(III) and Cu(II) complexes. Powder X-ray diffraction indicate the crystalline nature of the metal complexes. The antimicrobial activities of the Fe(III) and Cu(II) complexes were tested with various micro organisms by disc diffusion method. The antimicrobial results indicate that the metal complexes are highly active with compared to the free ligand. The in vitro antioxidant activity of the free ligand and its metal complexes was assayed by radical scavenging activity (DPPH). The result proposed that Fe (III) and Cu(II) complexes exhibited strong antioxidant activity than that of the ligand.

scholarly journals Novel Nonsymmetrically p-Benzyl-Substituted (Benz)imidazole N-Heterocyclic Carbene-Silver(I) Acetate Complexes: Synthesis and Biological Evaluation

2012 ◽  
Vol 2012 ◽  
pp. 1-13 ◽  
Author(s):  
Frauke Hackenberg ◽  
Anthony Deally ◽  
Grainne Lally ◽  
Sina Malenke ◽  
Helge Müller-Bunz ◽  
...  
Keyword(s):  
Cancer Cell Line ◽  
Benzyl Bromide ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
X Ray Diffraction ◽  
Gram Positive Bacteria ◽  
Acetate Complex ◽  
Renal Cancer Cell ◽  
Synthesis And Biological Evaluation

Nonsymmetrically substituted N-heterocyclic carbene (NHC) precursors 1a–d and 3a–d were synthesised by first reacting 1H-(benz)imidazole with p-cyanobenzyl bromide to give 4-(1H-imidazole-1-ylmethyl)benzonitrile (1) and 4-(1H-benzimidazole-1-ylmethyl)benzonitrile (3) and afterwards introducing benzyl bromide, 1-(bromomethyl)-4-methylbenzene, 1-(bromomethyl)-4-methoxybenzene, and methyl 4-(bromomethyl)benzoate. The NHC-silver(I) acetate complexes (1-benzyl-3-(4-cyanobenzyl)-2,3-dihydro-1H-imidazole-2-ylidene) silver(I) acetate (2a), (1-(4-cyanobenzyl)-3-(4-methylbenzyl)-2,3-dihydro-1H-imidazole-2-ylidene) silver(I) acetate (2b), (1-(4-cyanobenzyl)-3-[4-(methoxycarbonyl)benzyl]-2,3-dihydro-1H-imidazole-2-ylidene) silver(I) acetate (2c), (1-benzyl-3-(4-cyanobenzyl)-2,3-dihydro-1H-benzimidazole-2-ylidene) silver(I) acetate (4a), (1-(4-cyanobenzyl)-3-(4-methylbenzyl)-2,3-dihydro-1H-benzimidazole-2-ylidene) silver(I) acetate (4b), (1-(4-cyanobenzyl)-3-(4-methoxybenzyl)-2,3-dihydro-1H-benzimidazole-2-ylidene) silver(I) acetate (4c), and (1-(4-cyanobenzyl)-3-[4-(methoxycarbonyl)benzyl]-2,3-dihydro-1H-benzimidazole-2-ylidene) silver(I) acetate (4d) were yielded by reacting these NHC precursors with silver(I) acetate. The silver(I) acetate complex 4b was characterised by single crystal X-ray diffraction. Preliminary in vitro antibacterial studies against the Gram-positive bacteria Staphylococcus aureus and the Gram-negative bacteria Escherichia coli, using the Kirby-Bauer disc diffusion method, were carried out on the seven NHC-silver(I) acetate complexes 2a–c and 4a–d. Also the IC50 values of these seven complexes were determined by an MTT-based assay against the human renal cancer cell line Caki-1. The complexes 2a–c and 4a–c revealed the following IC50 values, respectively, 25 (±1), 15 (±2), 5.4 (±0.8), 16 (±2), 7.1 (±1), 20 (±4), and 14 (±1) μM.

scholarly journals Synthesis and Antimicrobial Activities of N-(Heteroaryl-substituted)-p-toluenesulphonamides

2014 ◽  
Vol 2014 ◽  
pp. 1-5
Author(s):  
Ozoh Chinwe Francisca ◽  
Okoro Uchechukwu Chris ◽  
Ugwu David Izuchukwu
Keyword(s):  
Biological Activities ◽  
Condensation Reaction ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Gram Positive Bacteria ◽  
New Class ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal ◽  
C Nmr

A new class of N-(heteroaryl-substituted)-p-toluenesulphonamides has been synthesized exhibiting antibacterial and antifungal properties. The condensation reaction of p-toluenesulphonyl chloride 1 with appropriate substituted amino pyridines 2a–g in acetone furnished N-(heteroaryl-substituted)-p-toluenesulphonamides 3a–g. These derivatives were characterized by IR, 1H-, and 13C-NMR spectroscopy and were screened in vitro against gram-positive bacteria, gram-negative bacteria, and fungi organisms using agar-diffusion method. Results indicated improved biological activities over reference drugs such as Tetracycline (TCN) and Fluconazole (FLU).

scholarly journals Synthesis, biological evaluation and molecular docking studies of new 2-ethoxy-4-{[3-alkyl(aryl)-4,5-dihydro-1H-1,2,4-triazol-5-on-4-yl]-azomethine}-phenyl benzenesulfonate derivatives on human aldose reductase enzyme

2021 ◽  
Author(s):  
Gül Özdemir ◽  
Namık Kılınç ◽  
Sevda Manap ◽  
Murat Beytur ◽  
Muzaffer Alkan ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antibacterial Activities ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Binding Energies ◽  
Diffusion Method ◽  
Alkyl Aryl ◽  
Molecular Docking Studies ◽  
New Compounds

A series of 2-ethoxy-4-{[3-alkyl(aryl)-4,5-dihydro-1H-1,2,4-triazol-5-on-4-yl]-azomethine}-phenyl benzenesulfonates (3) were synthesized from the reactions of 3-alkyl(aryl)-4-amino-4,5-dihydro-1H-1,2,4-triazol-5-ones (1) with 2-ethoxy-4-formyl-phenyl benzenesulfonate (2). N-acetyl derivatives (4) of compounds 3 were also obtained. Then, the compounds 3 have been treated with morpholine and 2,6-dimethylmorpholine in the presence of formaldehyde to synthesize 2-ethoxy-4-{[1-(morpholine-4-yl-methyl)-3-alkyl(aryl)-4,5-dihydro-1H-1,2,4-triazol-5-on-4-yl]-azomethine}-phenyl benzenesulfonates (5) and 2-ethoxy-4-{[1-(2,6-dimethylmorpholine-4-yl-methyl)-3-alkyl(aryl)-4,5-dihydro-1H-1,2,4-triazol-5-on-4-yl]-azomethine}-phenyl benzenesulfonates (6), respectively. The structures of twenty-six new compounds were identified by using elemental analysis, IR, 1H NMR, 13C NMR, and MS spectral data. In addition, in vitro antibacterial activities of the new compounds were evaluated against six bacteria such as Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis, Bacillus cereus and Klepsiella pneumonia according to agar well diffusion method. Furthermore, in order to determine the possible antidiabetic properties of the synthesized 1,2,4-triazole derivatives, inhibition effects on the AR enzyme were investigated and molecular docking studies were carried out to determine the receptor-ligand interactions of these compounds. IC50 values of triazole-derived compounds (6a, 6b, 6d-g) against AR enzyme were determined as 0.95 µM, 0.75 µM, 1.83 µM, 0.62 µM, 1.05 µM, 1.06 µM, respectively. Considering the docking scores and binding energies obtained docking studies, it has been shown that molecules fit very well to the active site of the AR enzyme.

scholarly journals Synthesis and biological evaluation of pyrazole analogues linked with 1,2,3-triazole and 4-thiazolidinone as antimicrobial agents

2022 ◽  
Vol 11 (1) ◽  
pp. 139-146 ◽  
Author(s):  
Nagaraj Adki ◽  
Neelofer Rana ◽  
Ramesh Naik Palthya
Keyword(s):  
Antimicrobial Agents ◽  
Micrococcus Luteus ◽  
Trichophyton Mentagrophytes ◽  
Biological Evaluation ◽  
Significant Activity ◽  
Standard Drug ◽  
Gram Positive Bacteria ◽  
Highly Active ◽  
In Vitro Antibacterial Activity

A new series of 2-[3-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)-1-phenyl-1H-4-pyrazolyl]-3-aryl-1,3-thiazolan-4-one 5(a-i) have been designed, synthesized and evaluated for their in vitro antibacterial activity against Gram positive bacteria viz. Bacillus subtilis (ATCC 6633), Staphylococcus aureus (ATCC 6538p), Micrococcus luteus (IFC 12708) and Gram negative bacteria viz. Proteus vulgaris (ATCC 3851), Salmonella typhimurium (ATCC 14028), Escherichia coli (ATCC 25922) the antifungal activity against Candida albicans (ATCC 10231), Aspergillus fumigatus (HIC 6094), Trichophyton rubrum (IFO 9185), Trichophyton mentagrophytes (IFO 40996). Antibacterial evaluation indicates that compounds containing 4-methoxyphenyl 5c, 4-fluorophenyl 5d and 2,5-difluorophenyl 5h groups on thiazolidinone ring showed significant activity equal to that of standard drug. The antifungal evaluation shows that compound 5c is highly active against A. fumigatus, compound 5d and 5h were also active against C. albicans and A. fumigatus.

scholarly journals In vitro Antibacterial Activity Analysis of Leaves of Limonia acidissima

2014 ◽  
Vol 6 (2) ◽  
pp. 155-157
Author(s):  
Gandi Kishore NAIDU ◽  
B. SUJATHA ◽  
K. Chandra Sekhar NAIDU
Keyword(s):  
Antibacterial Activity ◽  
Micrococcus Luteus ◽  
Chloroform Extract ◽  
Diffusion Method ◽  
Moderate Activity ◽  
Phytochemical Screening ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Limonia Acidissima

The present study was carried out the antibacterial activity and phytochemical screening of the hexane, chloroform and methanol extracts of leaves of Limonia acidissima. The antibacterial activity was evaluated against four Gram-negative (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Proteus vulgaris) and five Gram-positive bacteria (Bacillus subtilis, Enterococcus faecalis, Micrococcus luteus, Staphylococcus aureus, Streptococcus pneumoniae) by agar well diffusion method. Methanol extract showed good antibacterial activity with the high inhibition zones while chloroform extract exhibited mild to moderate activity and hexane extract was found to be less active. Phytochemical screening revealed the presence of various secondary metabolites like steroids, alkaloids, phenols, flavonoids, coumarins, saponins, tannins and triterpenoids. The results of the present study suggest that leaves of Limonia acidissima can be used to treating infectious diseases caused by E. coli, P. vulgarisand S. pneumoniae.

scholarly journals Synthesis, Characterization and Biological Evaluation of Metal(II) Complexes Containing Triphenylphosphine and Schiff Base Ligand Based on 3-Methoxysalicylaldehyde

2021 ◽  
Vol 33 (8) ◽  
pp. 1819-1823
Author(s):  
G. Gokulnath ◽  
P. Anitha ◽  
R. Manikandan ◽  
C. Umarani
Keyword(s):  
Schiff Base ◽  
Cancer Cell ◽  
Schiff Base Ligand ◽  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Gram Positive Bacteria ◽  
Antimicrobial Efficiency ◽  
Nmr Techniques

Schiff base ligand (HL) derived from condensation of 3-methoxy salicylaldehyde with 4-aminobenzoic acid and its metal(II) complexes containing triphenylphosphine of the type [MCl(PPh3)(L)] (M = Ni2+, Co2+ or Cu2+; L = bitendate Schiff base ligand) have been synthesized. All the metal(II) complexes were characterized by analytical and spectroscopic (FT-IR, electronic, ESI-Mass, ESR, 1H, 13C NMR and 31P NMR) techniques. All the synthesized compounds were evaluated for in vitro antimicrobial efficiency against Gram-positive bacteria, Gram-negative bacteria and fungai using the agar well diffusion method. Anticancer activity in vitro of the ligand and its metal(II) complexes were also screened against MCF-7 cancer cell lines (human breast cancer cell line).

scholarly journals Synthesis, Characterization and Biological Evaluation of Schiff Base (N-4-(thiophene-2-yl-methyleneamino)-2,6-dimethylpyrimidine-4-yl)benzenesulfonamide and its Complexes with Cu(II), Ni(II), Co(II), Fe(II), Mn(II), Zn(II) Ions

2020 ◽  
Vol 71 (1) ◽  
pp. 206-212 ◽  
Author(s):  
Amina Mumtaz ◽  
Tariq Mahmud ◽  
M. R. J. Elsegood ◽  
G. W. Weaver ◽  
Gabriel Bratu ◽  
...  
Keyword(s):  
Schiff Base ◽  
Transition Metal ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Schiff Base Ligand ◽  
Condensation Reaction ◽  
Klebsiella Oxytoca ◽  
Biological Evaluation ◽  
Anti Inflammatory

Two step synthesis of Schiff base ligand and its transition metal complexes was done by condensation reaction. In first step, the drug and aldehyde in equimolar ratio were refluxed for one hour at pH 8-9 in order to get Schiff base ligand. In second step, ligand and metal salts were refluxed for 2 hour. The ligand and Cu(II), Ni(II), Co(II), Fe(II), Mn(II), Zn(II) complexes were characterized by using different instruments like FT-IR, 1H-NMR, 13C-NMR, Mass, Atomic absorption spectrometer, Elemental analyzer, UV-visible spectrophotometer, Evans balance, Conductivitymeter and Thermogravimeter. In vitro antibacterial, antifungal and anti-inflammatory activities were also studied. The synthesized ligand and transition metal complexes were tested against Escherichia coli, Enterobacter aerogenes, Staphylococcus aureus, Bacillus pumilus, Klebsiella oxytoca, Clostridium butyrium, Mucor and Aspergillus niger. These studies demonstrated the enhanced activity of metal complexes against reported bacterial and fungal strains when compared with free Schiff base ligand. The Cu(II) complex recognized as anti-inflammatory agent while the parent drug showed no activity.

scholarly journals Synthesis, Characterization and Biological Evaluation of some Novel Substituted Indole-Coumarin Derivatives as Potential Antibacterial and Antifungal Agents

2021 ◽  
pp. 40-46
Author(s):  
Pallavi Kishor Vawhal ◽  
Shailaja B. Jadhav
Keyword(s):  
Candida Albicans ◽  
Antifungal Agents ◽  
Antibacterial Activities ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Coumarin Derivatives ◽  
Potato Dextrose Agar Medium ◽  
Fungal Strains ◽  
Antibacterial And Antifungal

Aim: In the present work, we have designed and synthesized indole-fused coumarin derivatives as potential antibacterial and antifungal agents. Place and Duration of Study: The present work was carried out at PEA's Modern college of Pharmacy, Sector 21, Yamunanagar, Nigdi- 411044 between the duration of January-2021 to May-2021. Methodology: The in vitro antibacterial and antifungal activity was performed by disc diffusion method. The antibacterial activities were tested using agar nutrient medium against Bacillus subtilis, Bacillus pumilus, Escherichia coli, and Pseudomonas aeruginosa that are representative types of gram-positive and gram-negative organisms respectively. The anti-fungal activity of all the compounds were determined on potato dextrose agar medium against Aspergillus niger and Candida albicans. Clotrimazole 100 μg/ml was used as a standard and DMF was used as control. Results: It was observed that all the compounds were sensitive to the gram +ve bacteria. Compound 2c, 2e, and 2f were sensitive to gram –ve bacteria. Compounds 2a, 2b, and 2f were sensitive to both the fungal strains while all the derivatives were sensitive to Candida albicans. Conclusion: From present investigation it has been observed that compound 2f was sensitive against gram +ve, gram –ve, and both the strains of fungal strains. Structurally, compound 2f possess aldehyde functional group at indole nucleus. Therefore, from present study we have concluded that compound 2f is a lead molecule for the further development of potential antibacterial and antifungal agents.

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