Synthesis and antimicrobial activity of 4-trifluoromethylpyridine nucleosides

2017 ◽  
Vol 23 (3) ◽  
pp. 197-203 ◽  
Author(s):  
Shaikha S. Alneyadi ◽  
Anas A. Abdulqader ◽  
Alaa A. Salem ◽  
Ibrahim M. Abdou
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Stenotrophomonas Maltophilia ◽  
Antibacterial Agents ◽  
Antibacterial Activities ◽  
Nucleoside Analogues ◽  
Reference Drug ◽  
Minimum Inhibitory Concentrations

Abstract4-Trifluoromethylpyridine derivatives 4–8 represent good candidates for the discovery of new antibacterial agents. Fluorinated pyridine nucleosides 4–7 and non-nucleoside analogues 8a,b were synthesized and evaluated for their antibacterial activities against Staphylococcus aureus, Bacillus infantis, Escherichia coli and Stenotrophomonas maltophilia. The minimum inhibitory concentrations (MICs) of the new nucleosides 4–7 range from 1.3 to 4.9 μg/mL and MICs of fluoroaryl derivatives 8a,b are in the range of 1.8–5.5 μg/mL. Activity of amoxicillin, the reference drug, is 1.0–2.0 μg/mL under similar conditions.

scholarly journals Oxidative Stress and Antimicrobial Activity of Chromium(III) and Ruthenium(II) Complexes onStaphylococcus aureusandEscherichia coli

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Paulina L. Páez ◽  
Claudia M. Bazán ◽  
María E. Bongiovanni ◽  
Judith Toneatto ◽  
Inés Albesa ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Antibacterial Agents ◽  
Antibacterial Activities ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
E Coli ◽  
Diimine Ligands

The prevalence of antibiotic resistance has resulted in the need for new approaches to be developed to combat previously easily treatable infections. The main aim of this work was to establish the potential of the syntheticα-diimine chromium(III) and ruthenium(II) complexes (where theα-diimine ligands are bpy = 2,2-bipyridine, phen = 1,10-phenanthroline, and dppz = dipyrido[3,2-a:2′,3′-c]-phenazine) like [Cr(phen)3]3+, [Cr(phen)2(dppz)]3+, [Ru(phen)3]2+, and [Ru(bpy)3]2+as antibacterial agents by generating oxidative stress. The [Cr(phen)3]3+and [Cr(phen)2(dppz)]3+complexes showed activity against Gram positive and Gram negative bacteria with minimum inhibitory concentrations (MICs) ranging from 0.125 μg/mL to 1 μg/mL, while [Ru(phen)3]2+and [Ru(bpy)3]2+do not exhibit antimicrobial activity against the two bacterial genera studied at the concentration range used. When ciprofloxacin was combined with [Cr(phen)3]3+for the inhibition ofStaphylococcus aureusandEscherichia coli, an important synergistic effect was observed, FIC 0.066 forS. aureusand FIC 0.064 forE. coli. The work described here shows that chromium(III) complexes are bactericidal forS. aureusandE. coli. Our results indicate thatα-diimine chromium(III) complexes may be interesting to open new paths for metallodrug chemotherapy against different bacterial genera since some of these complexes have been found to exhibit remarkable antibacterial activities.

scholarly journals Antioxidant and Antibacterial Activities of the Essential Oil of Moroccan Tetraclinis articulata (Vahl) Masters

2020 ◽  
Vol 2020 ◽  
pp. 1-6
Author(s):  
Halima Rabib ◽  
Chaimaa Elagdi ◽  
Mohammed Hsaine ◽  
Hassan Fougrach ◽  
Tayeb Koussa ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Essential Oil ◽  
Antioxidant Properties ◽  
Antibacterial Activities ◽  
Bornyl Acetate ◽  
Radical Trap ◽  
Tetraclinis Articulata

The purpose of this study is to evaluate and compare the antioxidant and antibacterial activities of essential oil isolated from Tetraclinis articulata (Vahl) leaves, Masters originating in Morocco (Benslimane Region, Atlantic-influenced plain). The analysis of the major compounds of essential oil was performed by gas chromatography and mass spectrometry, and this oil is dominated by bornyl acetate (35.05%), camphor (11.17%), and α-pinene (10.84%). The antioxidant properties were evaluated by the test of the radical trap 2,2-diphényl-1-picrylhydrazyl (DPPH), and the antimicrobial activity of T. articulata essential oil was tested against clinical isolates of Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli which have been inhibited from the 25 μg/mL.

Preparation and Antimicrobial Activity of Antibacterial Silver-Loaded Polyphosphazene Microspheres

2021 ◽  
Vol 21 (10) ◽  
pp. 5120-5130
Author(s):  
Hui Long ◽  
Wei-Cong Kuang ◽  
Shi-Liang Wang ◽  
Jing-Xian Zhang ◽  
Lang-Huan Huang ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Thermal Stability ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Silver Nanoparticles ◽  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Good Thermal Stability ◽  
Polymerization Method

Poly(cyclotriphosphazene-co-4,4’-diaminodiphenyl ether) (PPO) microspheres were prepared via a precipitation polymerization method, using hexachlorocyclotriphosphazene (HCCP) and 4,4’-diaminodiphenyl ether (ODA) as monomers. Silver-loaded PPO (PPOA) microspheres were generated by the in situ loading of silver nanoparticles onto the surface by Ag+ reduction. Our results showed that PPOA microspheres were successfully prepared with a relatively uniform distribution of silver nanoparticles on microsphere surfaces. PPOA microspheres had good thermal stability and excellent antibacterial activity towards Escherichia coli and Staphylococcus aureus. Furthermore, PPOA microspheres exhibited lower cytotoxicity when compared to citrate-modified silver nanoparticles (c-Ag), and good sustained release properties. Our data indicated that polyphosphazene-based PPOA microspheres are promising antibacterial agents in the biological materials field.

scholarly journals Comparative Antibacterial Efficacy of Vitellaria paradoxa (Shea Butter Tree) Extracts Against Some Clinical Bacterial Isolates

2015 ◽  
Vol 7 (3) ◽  
pp. 264-268 ◽  
Author(s):  
Kamoldeen Abiodun AJIJOLAKEWU ◽  
Fola Jose AWARUN
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Klebsiella Pneumoniae ◽  
Bacterial Pathogens ◽  
Stem Bark ◽  
Antibacterial Activities ◽  
Shea Butter ◽  
Vitellaria Paradoxa ◽  
Ethanolic Extracts

The antibacterial activities of the ethanolic extracts of seed, leaf and stem bark of Vitellaria paradoxa were investigated. The extracts were tested against three clinical bacterial pathogens, Staphylococcus aureus, Escherichia coli and Klebsiella pneumoniae using the agar diffusion and the broth dilution techniques. Ethanolic extracts of the plant parts showed activity against all the bacterial pathogens tested. At the highest extract concentration (200 mg/ml), the leaf extract exhibited the highest antimicrobial activity, while no activity was detected at the lowest concentration (3.13 mg/ml) against the tested isolates. Escherichia coli and Staphylococcus aureus were more susceptible to all extracts of V. paradoxa, while Klebsiella pneumoniae showed the least sensitivity. The efficacy of ethanolic extracts of Vitellaria paradoxa was compared to a commercial antibiotic streptomycin. There were differences in the minimum inhibitory concentration (MIC) of all the Vitellaria paradoxa ethanolic extracts with respect to the type of organism. All extracts exhibited bacteriostatic effects against the tested organisms at the experimented concentrations. Qualitative phytochemical screening of the extracts revealed the presence of saponins, tannins and alkaloids as the active principles of Vitellaria paradoxa's antimicrobial activity. V. paradoxa could be used as a potential source of antibiotic substance for a drug development.

scholarly journals Synthesis and Antibacterial Activities of Coumarins with an Acyl Amino Side Chain

2021 ◽  
Vol 68 (1) ◽  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Antibacterial Activities ◽  
Ring Structure ◽  
Coumarin Derivatives ◽  
Anti Cancer ◽  
Synthetic Reactions ◽  
Derivatives Of

Coumarin is a heterocyclic moiety containing benzo pyran ring structure. It is widely distributed in the plant kingdom as a glycoside. Many compounds of medicinal and pharmaceutical importance possess coumarin ring structure. Drugs with coumarin structure can be synthesized by many well-known synthetic reactions. Coumarin derivatives were found to be antibacterial, anticoagulant, antiinflammatory, anti-HIV, anti-cancer and antioxidant. As part of the search for new and effective antibacterial agents, eight novel derivatives of coumarins were synthesized by Mannich reaction. All the compounds were evaluated for antibacterial activity against Staphylococcus aureus and Escherichia coli using ciprofloxacin as standard and DMSO as solvent. Three of the synthesized derivatives exhibited good antibacterial activity against Staphylococcus aureus and Escherichia coli. The work must be extended so as to develop coumarin derivatives into highly effective antibacterial agents.

scholarly journals Synthesis, characterization and antimicrobial activity of novel benzofuran- and thiophene-containing diketoxime derivatives

2017 ◽  
Vol 82 (4) ◽  
pp. 367-377 ◽  
Author(s):  
Demet Coskun ◽  
Seher Gur ◽  
Mehmet Coskun
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Salmonella Enterica ◽  
Good Activity ◽  
E Coli ◽  
Minimum Inhibitory Concentrations ◽  
Serovar Typhimurium ◽  
And Staphylococcus Aureus

The aim of this study was the preparation of 1,1?-(2,5-thiophenediyl) bis[1-(2-benzofuranyl)methanone] (2), the corresponding diketoxime (3), and the ether and ester derivatives (4a?e) of the diketoxime. These compounds were prepared in good yields. Minimum inhibitory concentrations (MIC) of the synthesized compounds 1?4 were determined against Salmonella enterica subsp. enterica serovar Typhimurium, Escherichia coli and Staphylococcus aureus. Among the synthesized compounds, 1 and 4e showed good activity against E. coli, S. enterica and S. aureus.

scholarly journals Design, Synthesis and Antibacterial Activities of Triazole-pyrimidine Derivatives as SecA Inhibitors

2021 ◽  
Author(s):  
FANTE BAMBA ◽  
Tchambaga Camara ◽  
Coulibali Sioménan ◽  
Sagne Jacques Akpa ◽  
Adjou Ané
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Bacillus Anthracis ◽  
Structural Modification ◽  
Antibacterial Activities ◽  
Pyrimidine Derivative ◽  
Pyrimidine Derivatives ◽  
Design Synthesis ◽  
Secretion Pathway

Abstract SecA, a key component of bacterial Sec-dependent secretion pathway, is an attractive target for exploring novel antimicrobials. Along this line, we reported optimization of a hit bistriazole (SCA 21) which has been previously identified as a SecA inhibitor. Herein we describe the synthesis of some novel triazole-pyrimidine derivative by structural modification of SCA 21. Some of them have been evaluated for their antimicrobial activity against against Escherichia coli NR698 (a leaky mutant), Staphylococcus aureus and Bacillus anthracis Sterne.

Metal-Polymer Complexes as Antibacterial Agents: Characterization and Antibacterial Activity of Metal-Polymer Nanocomposite Based on Copolymers of Polyethylene(Propylene)Glycolmaleates with Acrylic Acid

2022 ◽  
Author(s):  
T.O. KHAMITOVA ◽  
M.ZH. BURKEEV ◽  
A.ZH.SARSENBEKOVA ◽  
M.YU. ISHMURATOVA ◽  
G.K.MUKUSHEVA ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Acrylic Acid ◽  
Antibacterial Agents ◽  
High Efficiency ◽  
Polymer Nanocomposite ◽  
Polymer Complexes ◽  
Structure Of Metal ◽  
Metal Polymer

Abstract The article presents the results of the synthesis and study of the structure of metal-polymer complexes p-EGM: АА/Ag, p-EGM: АА/Ni, p-EGM:АА/Ag-Ni, p-PGM:АА/Ag, p-PGM:АА/Ni, p-PGM:АА/Ag-Ni based on copolymers of polyethylene(propylene)glycolmaleates with acrylic acid and metals, which have been characterized using microscopy, spectroscopy and thermogravimetry. The antimicrobial activity of a new metal-polymer nanocomposite p-PGM/АА-Ag was studied, which is showing high efficiency against standard strains of Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus.

scholarly journals Chemical Composition and Antimicrobial Activity of Essential Oils of Genista ulicina and G. vepres

2010 ◽  
Vol 5 (5) ◽  
pp. 1934578X1000500 ◽  
Author(s):  
Takia Lograda ◽  
Adel Nadjib Chaker ◽  
Jean Claude Chalchat ◽  
Messaoud Ramdani ◽  
Hafsa Silini ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Antibacterial Activities ◽  
Gas Chromatography Mass Spectrometry ◽  
Diffusion Method ◽  
Aerial Parts ◽  
Total Oil ◽  
And Staphylococcus Aureus

The hydrodistilled oils from the aerial parts of Genista ulicina Spach. and G. vepres Pomel., which are endemic to Algeria, were analyzed by gas chromatography-mass spectrometry (GC-MS). In the oil of G. ulicina, 41 compounds were identified representing 90.8% of the total oil, and in G. vepres, 61 compounds representing 84.5% of the total oil. The analyses showed that the major constituents of the oils were lauric acid (14.3% – 8.5%), myristic acid (11.5% – 5%), linoleic acid (3.1% –11.7%) and palmitic acid (18.6% – 26.4%). Using a diffusion method, the oils showed significant antibacterial activities against Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853) and Staphylococcus aureus (ATCC 25923).

scholarly journals COMPARATIVE ANTIMICROBIAL ACTIVITY OF FIVE BRANDS OF CIPROFLOXACIN SOLD IN LAGOS STATE

2017 ◽  
Vol 15 (1) ◽  
pp. 21-32
Author(s):  
B. A. ADENIYI ◽  
C. I. AYOLABI ◽  
E. J. UKONU
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Bactericidal Activity ◽  
Salmonella Enterica ◽  
Antibacterial Activities ◽  
Test Organisms ◽  
Concentration Test ◽  
The Mean ◽  
Made In

he antimicrobial activity of five brands (A, B, C, D and E) of ciprofloxacin hydrochloride tablets commonly sold in Lagos Nigeria, were compared and assessed against susceptible clinical isolates (Staphylococcus aureus, Escherichia coli and Salmonella enterica serotypetyphi). Susceptibility test, minimum inhibitory concentration test and the bactericidal activity were determined. All sampled brands were within their shelf life. Most (60%) of the sampled brands were made in India while the remaining 40% were made in Nigeria. All the brands complied with the official specification in British Pharmacopeia (BP) for uniformity of weight as they show less than 5% deviation in weight. The mean antibacterial activities of the brands at 25µg/ml were found to be within the range of 38.0mm to 42.2mm zone of inhibition while the MICs range between 0.012µg/ml to 1.5µg/ml.All the sampled brands were effective against all the test organisms to varying degree with brands A and E been more potent while brand D was the least effective. The order of MICs (decreasing order of potency) was D>B>C>A>E for Staphylococcus aureus and D>C>B>E>A for Escherichia coli while that of Salmonella enterica serotypeTyphiwas D>B>C>A>E. The bactericidal activity of each ciprofloxacin brand D and E are concentration-dependent; with brand E more active at all tested concentrations. 

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