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.

scholarly journals Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1339 ◽  
Author(s):  
Islam H. El Azab ◽  
Nadia A.A. Elkanzi
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Positive Control ◽  
Design Synthesis ◽  
Aspergillus Brasiliensis ◽  
In Vitro Investigation ◽  
Bacillus Subtilis Atcc ◽  
Antimicrobial Evaluation

A series of 34 new pyrimido[2,1-c][1,2,4]triazine-3,4-diones were synthesized and fully characterized using IR, NMR, MS, and microanalytical analysis. In vitro investigation of 12 compounds of this series revealed promising antimicrobial activity of the conjugates 15a and 15f–j that were tagged with electron-withdrawing groups, with sensitivities ranging from 77% to as high as 100% of the positive control. The investigation of antimicrobial activity included Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 6535, Pseudomonas aeruginosa ATCC 27853, and Escherichia coli ATCC 8739 (EC), and fungal strains Candida albicans ATCC 10231 and Aspergillus brasiliensis ATCC 16404.

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 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.

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 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 Solid Phase Synthesis and Antimicrobial Activity of Novel Triazolo[1,5-a]pyrimidine Derivatives

2020 ◽  
Vol 32 (9) ◽  
pp. 2298-2302
Author(s):  
SHOBHANA A. GADARA ◽  
KARTIK D. LADVA
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Dilution Method ◽  
Pyrimidine Derivatives ◽  
Phase Synthesis ◽  
Inhibition Concentration ◽  
Broth Dilution

A new series of triazolo[4,3-a]pyimidine derivatives via solid phase multicomponent reaction between 3-oxo-N-(4-(3-oxomorpholino)- phenyl)butanamide, aromatic aldehyde and aminoazole is reported. All the synthesized compounds have been characterized by elemental analysis and spectral analyses. Moreover, the synthesized compounds were also screened for their antibacterial activity against Staphylococcus aureus MTCC-96, Escherichia coli MTCC-443, Bacillus subtilis MTCC-441, Pseudomonas aeruginosa MTCC 1688, and antifungal activity against Aspergillus niger MTCC-282 and Penicillium sp. at different concentration and compared with standards drugs. The minimum inhibition concentration (MIC) of the compounds was studied by micro-broth dilution method.

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. 

Screening and antimicrobial activity of actinomycetes isolated from the rhizosphere of Clitoria ternatea

2016 ◽  
Vol 1 (01) ◽  
Author(s):  
Vemavarapu Bhaskara Rao ◽  
Kandlagunta Guru Prasad ◽  
Krishna Naragani ◽  
Vijayalakshmi Muvva
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Candida Albicans ◽  
Calcium Carbonate ◽  
Rhizosphere Soil ◽  
Soil Samples ◽  
Antimicrobial Spectrum ◽  
Clitoria Ternatea ◽  
Primary Screening

The air dried rhizosphere soil samples pretreated with calcium carbonate was employed for the isolation of actinomycete strains. Serial dilution plate technique was used for the isolation of actinomycetes. A total of 20 actinomycete strains designated as BS1-BS20 were isolated from the rhizosphere of medicinal plant Clitoria ternatea. All the 20 strains were subjected to primary screening for antimicrobial activity. Among the 20 strains screened, 10 strains exhibited high antimicrobial spectrum against Staphylococcus aureus, Escherichia coli and Candida albicans.

Synthesis, photosensitization and antimicrobial activity evaluation of some novel Merocyanine dyes

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Aspergillus Flavus ◽  
Elemental Analysis ◽  
Cyanine Dyes ◽  
Fungal Strains ◽  
Activity Evaluation ◽  
Visible Spectra ◽  
Merocyanine Dyes

Novel acyclic and cyclic merocyanine dyes derived from the nucleu of furo [(3,2-d) pyrazole; ( d 2 , 3 )imidazole]were prepared. The electronic visible absorptionspectra of all the synthesized new cyanine dyes were examined in 95% ethanolsolution to evaluate their photosensitization properties. Antibacterial andantifungal activities for some selected dyes were tested against various bacterialand fungal strains (Escherichia coli, Staphylococcus aureus, Aspergillus flavus andCandida albicans) to evaluate their antimicrobial activity. Structural identificationwas carried out via elemental analysis, visible spectra, IR and 1H NMRspectroscopic data.

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