scholarly journals Synthesis and Biological Evaluation of Benzo[b]thiophene Acylhydrazones as Antimicrobial Agents against Multidrug-Resistant Staphylococcus aureus

Biomolecules ◽  
2022 ◽  
Vol 12 (1) ◽  
pp. 131
Author(s):  
Thibaut Barbier ◽  
Alexia Barbry ◽  
Jérémy Magand ◽  
Cédric Badiou ◽  
Floriane Davy ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Minimal Inhibitory Concentration ◽  
Aromatic Ring ◽  
Antimicrobial Agents ◽  
Functional Group ◽  
Inhibitory Concentration ◽  
Multidrug Resistant ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Structural Diversification

The benzo[b]thiophene nucleus and the acylhydrazone functional group were combined to prepare three new series of compounds for screening against Staphylococcus aureus. The reaction of substituted benzo[b]thiophene-2-carboxylic hydrazide and various aromatic or heteroaromatic aldehydes led to a collection of 26 final products with extensive structural diversification on the aromatic ring and on position 6 of the benzo[b]thiophene nucleus. The screening lead to the identification of eight hits, including (E)-6-chloro-N’-(pyridin-2-ylmethylene)benzo[b]thiophene-2-carbohydrazide (II.b), a non-cytotoxic derivative showing a minimal inhibitory concentration of 4 µg/mL on three S. aureus strains, among which were a reference classical strain and two clinically isolated strains resistant to methicillin and daptomycin, respectively.

scholarly journals Synthesis and biological evaluation of some new 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines as antimicrobial agents

2022 ◽  
Vol 11 (1) ◽  
pp. 75-82 ◽  
Author(s):  
Iryna Myrko ◽  
Taras Chaban ◽  
Vasyl Matiychuk
Keyword(s):  
Mass Spectrometry ◽  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Synthesis And Biological Evaluation

A series of some new pyrazole-substituted 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines was synthesized in this study. The structures of target substances were confirmed by using 1H and 13С NMR spectroscopy, mass spectrometry and elemental analysis. The synthesized compounds have been evaluated for 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 screening studies of synthesized substances established that 2 of 12 compounds show pronounced antibacterial activity against the strain Staphylococcus aureus.

scholarly journals New Mechanism of Magnolol and Honokiol from Magnolia officinalis against Staphylococcus aureus

2014 ◽  
Vol 9 (9) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Tao Liu ◽  
Yalin Pan ◽  
Renfu Lai
Keyword(s):  
Staphylococcus Aureus ◽  
Cell Division ◽  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Multidrug Resistant ◽  
Binding Energies ◽  
Methicillin Resistant ◽  
Computer Aided ◽  
Cell Division Protein ◽  
Magnolia Officinalis

Cell division protein, FtsZ, has been identified as a new potential antimicrobial target against multidrug-resistant (MDR) and methicillin-resistant Staphylococcus aureus (MRSA). By using computer-aided simulation, the phenolic compounds magnolol and honokiol from Magnolia officinalis were shown to have high anchor energies to FtsZ of S.aureus. The calculated binding energies of magnolol and honokiol for this FtsZ (PDB Code: 4DXD) were established to be −7.6 kcal/mol and −8.2 kcal/mol, respectively. Both of them showed polymerization inhibition efficacy for this FtsZ at 100 ppm, which confirmed the simulation results. Their antibacterial activity against S. aureus including multidrug-resistant (MDR) and methicillin-resistant S.aureus (MRSA) with minimum inhibitory concentration (MIC) values in the range of 8–16 ppm. These findings support the use of computer-aided simulation to screen natural compounds for this cell division protein, FtsZ, and this method can be a quick and promising approach for the development of antimicrobial agents against multi-drug resistant S. aureus.

scholarly journals Inhibitory Activity of Levofloxacin against MDR Staphylococcus aureus and Pseudomonas aeruginosa Clinical Isolates

2019 ◽  
Vol 6 (1) ◽  
pp. 25
Author(s):  
Lisa Nathalie ◽  
Lindawati Alimsardjono ◽  
Isnaeni Isnaeni
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Minimum Inhibitory Concentration ◽  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Multidrug Resistant ◽  
Bacterial Concentration ◽  
Important Species ◽  
One Step

Introduction: Staphylococcus  aureus  and  Pseudomonas  aeruginosa  are the most dangerous  and important species among  their genus.  These  bacteria  are often  resistant  to  many  classes  of antimicrobial  agents;  which  make difficulties in selecting appropriate drug to treat infections. Multidrug-resistance occurs readily in hospitals for which antimicrobials  agents  were   used  widely. Objective: The  aims  of  this  study  was  to  determine  minimum  inhibitory concentration  (MIC) and  minimum bacterial  concentration  (MBC) of levofloxacin  against 22 multidrug  resistant- clinical (MDR) strains of Staphylococcus aureus and Pseudomonas aeruginosa isolated from patients pus and urine in hospital. Methods: Determination of the MIC was performed by macro-dilution broth assay as recommended by Clinical and Laboratory Standards Institute (CLSI), while the MBC was determined one-step further after the MIC determination. Results: It was found that MIC of the levofloxacin were (0.3 ± 0.0) - >0.5 µg/mL and (0.2 ± 0.1) - (1.0 ±0.0)µg/mL against S. aureus from pus and urine, respectively.  In addition, higher MICs were yielded against P. aeruginosa, (1.0 ± 0.0) - >8.0 µg/mL and (0.7 ± 0.3) - (3.0 ± 1.2) µg/mL for pus and urine isolates respectively. Similar to MICs, the MBCs against P. aeruginosa were higher than S. aureus, (0.6 ± 0.0) - > 4.0 µg/mL and (0.3 ± 0.0) - >8.0 µg/mL isolated from pus and urine respectively, (2.0 ± 0.6) - > 8.0 µg/mL and (3.0 ± 1.2) - >7.0 µg/mL against P. aeruginosa from pus and urine respectively. Conclusion: The levofloxacin was still susceptible as bacteriostatic against isolates from both body fluids, but not bactericidal towards all isolates.

Biological Evaluation of Selected 1,2,3-triazole Derivatives as Antibacterial and Antibiofilm Agents

2020 ◽  
Vol 20 (24) ◽  
pp. 2186-2191
Author(s):  
Lialyz Soares Pereira André ◽  
Renata Freire Alves Pereira ◽  
Felipe Ramos Pinheiro ◽  
Aislan Cristina Rheder Fagundes Pascoal ◽  
Vitor Francisco Ferreira ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Scanning Electron Microscopy ◽  
Staphylococcus Aureus ◽  
Biofilm Formation ◽  
Antimicrobial Agents ◽  
Public Health Problem ◽  
Biological Evaluation ◽  
Major Public Health Problem ◽  
Community Environments ◽  
Scanning Electron

Background: Resistance to antimicrobial agents is a major public health problem, being Staphylococcus aureus prevalent in infections in hospital and community environments and, admittedly, related to biofilm formation in biotic and abiotic surfaces. Biofilms form a complex and structured community of microorganisms surrounded by an extracellular matrix adhering to each other and to a surface that gives them even more protection from and resistance against the action of antimicrobial agents, as well as against host defenses. Methods: Aiming to control and solve these problems, our study sought to evaluate the action of 1,2,3- triazoles against a Staphylococcus aureus isolate in planktonic and in the biofilm form, evaluating the activity of this triazole through Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) tests. We have also performed cytotoxic evaluation and Scanning Electron Microscopy (SEM) of the biofilms under the treatment of the compound. The 1,2,3-triazole DAN 49 showed bacteriostatic and bactericidal activity (MIC and MBC 128 μg/mL). In addition, its presence interfered with the biofilm formation stage (1/2 MIC, p <0.000001) and demonstrated an effect on young preformed biofilm (2 MICs, p <0.05). Results: Scanning Electron Microscopy images showed a reduction in the cell population and the appearance of deformations on the surface of some bacteria in the biofilm under treatment with the compound. Conclusion: Therefore, it was possible to conclude the promising anti-biofilm potential of 1,2,3-triazole, demonstrating the importance of the synthesis of new compounds with biological activity.

Acinetobacter species in laboratory mice: species survey and antimicrobial resistance

2018 ◽  
Vol 53 (5) ◽  
pp. 470-477
Author(s):  
Laurentiu Benga ◽  
Andrea T. Feßler ◽  
W. Peter M. Benten ◽  
Eva Engelhardt ◽  
Karl Köhrer ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Rpob Gene ◽  
Multidrug Resistant ◽  
Laboratory Mice ◽  
Hospital Epidemiology ◽  
Acinetobacter Species ◽  
Acinetobacter Spp ◽  
Susceptibility Profiles ◽  
Very High

The extra-hospital epidemiology of Acinetobacter infections is a subject of debate. In recent years, the prevalence of animal multidrug-resistant Acinetobacter infections has increased considerably. The goal of the present study was to specify Acinetobacter species isolated from laboratory mice and to test them for their antimicrobial susceptibility. During routine microbiological monitoring of laboratory mice, 12 Acinetobacter spp. were isolated. By means of 16S rRNA and rpoB gene sequencing, seven of the isolates were identified as Acinetobacter radioresistens, three isolates belonged to Acinetobacter genomospecies 14BJ, one isolate was classified as Acinetobacter pitii and one as Acinetobacter sp. ANC 4051. The distribution of the minimal inhibitory concentration (MIC) values was uniform for 21 of the 23 antimicrobial agents tested, whereas a broad MIC distribution was recorded for tulathromycin and streptomycin. The MIC values recorded were low for the majority of the antibiotics tested. Nevertheless, very high MIC values, which will probably render a therapeutic approach using these substances unsuccessful, were recorded for florfenicol, tiamulin, tilmicosin and cephalothin in most of the isolates. In conclusion, we document colonization of laboratory mice with different Acinetobacter species, displaying similar antibiotic susceptibility profiles, with possible implications in the Acinetobacter epidemiology as well as in the husbandry and experimentation of the colonized animals.

scholarly journals Activity of Debio1452, a FabI Inhibitor with Potent Activity against Staphylococcus aureus and Coagulase-Negative Staphylococcus spp., Including Multidrug-Resistant Strains

2015 ◽  
Vol 59 (5) ◽  
pp. 2583-2587 ◽  
Author(s):  
Robert K. Flamm ◽  
Paul R. Rhomberg ◽  
Nachum Kaplan ◽  
Ronald N. Jones ◽  
David J. Farrell
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Agents ◽  
Fatty Acid Biosynthesis ◽  
Multidrug Resistant ◽  
Coagulase Negative Staphylococcus ◽  
Significant Activity ◽  
Coagulase Negative Staphylococci ◽  
Content Type ◽  
Mrsa Strains ◽  
Human Infections

ABSTRACTStaphylococcus aureusand coagulase-negative staphylococci (CoNS) are responsible for a wide variety of human infections. The investigational antibacterial Debio1450 (previously AFN-1720), a prodrug of Debio1452 (previously AFN-1252), specifically targets staphylococci without significant activity against other Gram-positive or Gram-negative species. Debio1452 inhibits FabI, an enzyme critical to fatty acid biosynthesis in staphylococci. The activity of Debio1452 against CoNS, methicillin-susceptibleS. aureus(MSSA), and methicillin-resistantS. aureus(MRSA), including significant clones, was determined. A globally diverse collection of 574 patient isolates from 35 countries was tested that included CoNS (6 species, 103 strains), MSSA (154 strains), MRSA (163 strains), and molecularly characterized strains (includingspa-typed MRSA clones; 154 strains). The isolates were tested for susceptibility by CLSI broth microdilution methods against Debio1452 and 10 comparators. The susceptibility rates for the comparators were determined using CLSI and EUCAST breakpoint criteria. AllS. aureusand CoNS strains were inhibited by Debio1452 concentrations of ≤0.12 and ≤0.5 μg/ml, respectively. The MIC50s for MSSA, MRSA, and molecularly characterized MRSA strains were 0.004 μg/ml, and the MIC90s ranged from 0.008 to 0.03 μg/ml. The MICs were higher for the CoNS isolates (MIC50/90, 0.015/0.12 μg/ml). AmongS. aureusstrains, resistance was common for erythromycin (61.6%), levofloxacin (49.0%), clindamycin (27.6%), tetracycline (15.7%), and trimethoprim-sulfamethoxazole (7.0%). Debio1452 demonstrated potent activity against MSSA, MRSA, and CoNS. Debio1452 showed significantly greater activity overall (MIC50, 0.004 μg/ml) than the other agents tested against these staphylococcal species, which included dominant MRSA clones and strains resistant to currently utilized antimicrobial agents.

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