scholarly journals In Vitro, Controlling the Establishment of Xanthomonas Campestris with different Bacterial Bioagents

2016 ◽  
Vol 29 (1) ◽  
pp. 37-40
Author(s):  
Amna Ali ◽  
M Saleem Haider ◽  
Sobia Mushtaq ◽  
Ibatsam Khokhar ◽  
Irum Mukhtar ◽  
...  
Keyword(s):  
Xanthomonas Campestris ◽  
Fruits And Vegetables ◽  
Antimicrobial Agents ◽  
Bacterial Species ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
Diffusion Technique

The antimicrobial agents of bacteria isolated from different rhizosphere of fruits and vegetables soil in Lahore. Of ten species, five were gram-negative (Escherichia coli, Pseudomonas fluorescence, Klebsiella pneumoniae, Salmonella typhii, Brachybacterium faecium); other five were gram positive and identified as Bacillus farraginis, Kurthia gibsonii, Aureobacterium liquefaciens, Curtobacterium albidum, Micrococcus lylae. The antagonistic potential of bacterial strains was assessed by the well diffusion technique and results indicating varying degree of biocontrol activity against pathogenic strain of X. campestris. Out of ten bacterial species, E. coli (gram negative) and C. albidum (gram positive) showed a high prevalence of resistance with reduction of 4.2cm and 4.1cm zone diameter respectively. The minimum inhibitory volume (MIV) to two bio-agents was determined for X. campestris from range 10-100 ?L. E. coli (volume required to inhibit < 20 ?L) and C. albidum (volume required to inhibit < 40 ?L) exhibited good activity against pathogen. These results provide information on the prevalence of resistant bacterial strains with the MIV of organisms and indicate the possibility of using these bacterial species as bio-agent against X. campestris.Bangladesh J Microbiol, Volume 29, Number 1, June 2012, pp 37-40

scholarly journals Synthesis and Antimicrobial Evaluations of Sulfur Inserted Fluoro-Benzimidazoles

2021 ◽  
Vol 33 (7) ◽  
pp. 1525-1529
Author(s):  
Parmesh Kumar Dwivedi ◽  
Devdutt Chaturvedi
Keyword(s):  
Antimicrobial Agents ◽  
Bacterial Strains ◽  
Substituted Anilines ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
New Compounds ◽  
Derivatives Of ◽  
Multiple Step

A new series of fluorinated sulfur inserted benzimidazole analogues Za-i were synthesized and characterized. The new compounds were screened for their antimicrobial and antioxidant potential. The synthesized compounds were obtained by multiple step synthesis, initiating from the synthesis of 5-(difluoromethoxy)-1H-benzimidazole-2-thiol X. The compounds Ya-i prepared by reacting differently substituted anilines with chloroacetylchloride and triethylamine in DMF. Finally, the compound X was reacted with different derivatives of 2-chloro-N-phenylacetamide resulting in formation of titled compounds Za-i. The synthesized compounds (Za-Zi) were characterized by spectral analysis viz.1H & 13C NMR, mass spectra, elemental analysis and IR. The in vitro antimicrobial potential against Gram-positive (S. aureus and E. faecalis) and Gram-negative bacterial (E. coli and P.aeruginosa) strains as well as fungi (A. niger and C. albicans) was recorded for the obtained compounds. Some of the compounds exhibited encouraging results (in MIC) against Gram-positive and Gram-negative bacterial strains. These studies thus suggest that the designed sulfur inserted fluoro-benzimidazoles scaffold may serve as new promising template for further amplification as antimicrobial agents.

Molecular Drug Design, Synthesis and Antibacterial study of Novel 4-Oxothiazolidin-3-yl Derivatives

2020 ◽  
pp. 1-10
Keyword(s):  
Antimicrobial Agents ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Design Synthesis ◽  
Gram Negative ◽  
Docking Simulations ◽  
Chemical Structures ◽  
Molecular Core ◽  
Diffusion Technique

New compounds containing 4-thiazolidinone pharmacophore 5(a) and (5b) have been synthesized. The chemical structures of the intermediate and final compounds were characterized and confirmed by using FT-IR and 1H-NMR spectroscopy. All final compounds were tested against gram-positive and gram-negative bacteria using a well-diffusion technique for their ability as antimicrobial agents. The tested compounds 5a and 5b showed variable and modest antibacterial activity against gram-negative bacteria and gram-positive bacteria. Molecular docking simulations were studied to understand the molecular core. The results were achieved by docking, the most active compounds into the active site of protein of the bacteria which completely accorded with in vitro results.

scholarly journals Design, Synthesis, and Antibacterial Screening of Some Novel Heteroaryl-Based Ciprofloxacin Derivatives as DNA Gyrase and Topoisomerase IV Inhibitors

2021 ◽  
Vol 14 (5) ◽  
pp. 399
Author(s):  
Lamya H. Al-Wahaibi ◽  
Amer A. Amer ◽  
Adel A. Marzouk ◽  
Hesham A.M. Gomaa ◽  
Bahaa G. M. Youssif ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Dna Gyrase ◽  
Bacterial Strains ◽  
Topoisomerase Iv ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
Antibacterial Screening ◽  
Ic50 Values

A novel series of ciprofloxacin hybrids comprising various heterocycle derivatives has been synthesized and structurally elucidated using 1H NMR, 13C NMR, and elementary analyses. Using ciprofloxacin as a reference, compounds 1–21 were screened in vitro against Gram-positive bacterial strains such as Staphylococcus aureus and Bacillus subtilis and Gram-negative strains such as Escherichia coli and Pseudomonas aeruginosa. As a result, many of the compounds examined had antibacterial activity equivalent to ciprofloxacin against test bacteria. Compounds 2–6, oxadiazole derivatives, were found to have antibacterial activity that was 88 to 120% that of ciprofloxacin against Gram-positive and Gram-negative bacteria. The findings showed that none of the compounds tested had antifungal activity against Aspergillus flavus, but did have poor activity against Candida albicans, ranging from 23% to 33% of fluconazole, with compound 3 being the most active (33% of fluconazole). The most potent compounds, 3, 4, 5, and 6, displayed an IC50 of 86, 42, 92, and 180 nM against E. coli DNA gyrase, respectively (novobiocin, IC50 = 170 nM). Compounds 4, 5, and 6 showed IC50 values (1.47, 6.80, and 8.92 µM, respectively) against E. coli topo IV in comparison to novobiocin (IC50 = 11 µM).

scholarly journals Antibacterial Activity of Floral Petals of Some Angiosperms

2019 ◽  
pp. 1-5 ◽  
Author(s):  
L. Rajanna ◽  
N. Santhosh Kumar ◽  
N. S. Suresha ◽  
S. Lavanya
Keyword(s):  
Antibacterial Activity ◽  
Pathogenic Bacteria ◽  
Inhibition Zone ◽  
Bacterial Strains ◽  
Inhibitory Zone ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
Antibacterial Assay

The in vitro antibacterial assay was carried out against both Gram positive (B. cerus and S. aureus) and Gram negative (E. coli and K. pneumoniae) bacteria. Floral petals of 20 different species of plants were collected and tested for antibacterial activity. The result showed that the petals were active against both Gram positive and Gram negative. Out of 20 floral petals tested, 19 floral petals exhibited antibacterial activity against selected bacterial strains. The minimal inhibitory zone of floral petal discs against human pathogenic bacteria varies from 2 – 6 mm. Rosa carolina and Ruellia tuberosa showed significance inhibition zone for all the bacterial strains while Lantana camara does not show inhibition zone for any of these pathogenic bacteria.

scholarly journals Design, Synthesis, and Evaluation of Novel 3-, 4-substituted, and 3,4-di Substituted Quinazoline Derivatives as Antimicrobial Agents

2020 ◽  
Vol 71 (2) ◽  
pp. 422-435
Author(s):  
Farag A. El-Essawy ◽  
Abdulrahman I. Alharthi ◽  
Mshari A. Alotaibi ◽  
Nancy E. Wahba ◽  
Nader M. Boshta
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Design Synthesis ◽  
Gram Negative ◽  
Spectroscopic Analyses ◽  
Quinazoline Derivatives

A novel series of 3-, 4-substituted, and 3,4-di substituted quinazoline derivatives were prepared via various cyclized regents and most of the newly prepared compounds evaluated for their antimicrobial activities in vitro against Gram-positive, Gram-negative bacterial strains and fungi strains. The structures of the quinazoline derivatives have been confirmed using spectroscopic analyses (IR, NMR, and EI-MS). Some of the synthesized derivatives displayed a moderate antimicrobial activity in comparison with reference drugs, for example compounds 13d, 15a, 17b, 18b, 18d, 25, and 29a-c. Among the synthesized compounds, the pyrimidoqunazoline derivative 6c elicited the highest activity.

scholarly journals Synthesis and antimicrobial activity of some new N-(aryl-oxo-alkyl)-5-arylidene-thiazolidine-2,4-diones

2014 ◽  
Vol 79 (2) ◽  
pp. 115-123 ◽  
Author(s):  
Anca Stana ◽  
Brînduşa Tiperciuc ◽  
Mihaela Duma ◽  
Adrian Pîrnău ◽  
Philippe Verité ◽  
...  
Keyword(s):  
Antimicrobial Activities ◽  
Fungal Strain ◽  
Gram Negative Bacteria ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Reference Drug ◽  
Gram Negative ◽  
E Coli ◽  
Inhibitory Activities

A series of new 5-(2,6-dichlorobenzylidene)thiazolidine-2,4-dione and 5-(4-methoxy-benzylidene)thiazolidine-2,4-dione derivatives (3a-h and 5a-h) were synthesized starting from 5-arylidene-thiazolidine-2,4-dione and ?-halo-ketones. The structural elucidation of the newly synthesized compounds was based on elemental analysis and spectroscopic data (MS, 1H-NMR, 13C-NMR). The synthesized compounds were screened for their antimicrobial activities against several pathogenic strains of Gram-positive and Gram-negative bacteria and one fungal strain (Candida albicans), assessed in vitro as growth inhibition diameters. Some of them displayed better inhibitory activities than that of the reference drug against the Gram-positive S. aureus, B. cereus, L. monocytogenes bacterial strains, and showed good antifungal activity against C. albicans, while the antibacterial activity against Gram-negative E. coli and S. typhimurium bacterial strains was moderate.

Synthesis and Characterization of Novel 1,3,5-Thiadiazine Derivatives Integrated with Quinoline Moiety as Potent Antimicrobial Agents

2020 ◽  
Vol 5 (2) ◽  
pp. 149-155
Author(s):  
M. Idrees ◽  
Naqui J. Siddiqui ◽  
Yogita G. Bodkhe ◽  
Satish Kola
Keyword(s):  
13C Nmr ◽  
Mass Spectra ◽  
Antimicrobial Agents ◽  
Synthesis And Characterization ◽  
Pathogenic Microorganism ◽  
Bacterial Strains ◽  
Gram Negative ◽  
E Coli

An expeditious synthesis of series of novel 1,3,5-thiadiazine (5a-f) and (6a-f) derivatives have been described. These compounds were synthesized by reaction of 1-(N-((6-methyl-2-(p-tolyloxy)quinoline- 3-yl)methylene)carbamimidoyl)-3-arylthiourea (3a-b) derivatives with N-aryl isocyanodichloride (4a-c) in chloroform followed by basification with dilute NH4OH to give the target compounds 5a-f; which were acetylated further to afford six novel 1,3,5-thiadiazin-3-(6H)-yl)ethanone (6a-f) derivatives. Synthesis of intermediate compounds 3a-b was obtained by reacting 6-methyl-2-(p-tolyloxy)quinoline-3- carbaldehyde (2a) and 1-carbamimidoyl-3-aryllthiourea (1a-b) in chloroform. Structures of compounds 5a-f and 6a-f were established by FTIR, 1H & 13C NMR, mass spectra and further supported by elemental analysis. All synthesized compounds were investigated for their in vitro antimicrobial screening against a panel of pathogenic microorganism comprising S. aureus as Gram positive while E. coli, P. vulgaris, S. typhi as Gram-negative bacterial strains.

scholarly journals Protamine-like proteins have bactericidal activity. The first evidence in Mytilus galloprovincialis

2018 ◽  
Author(s):  
Rosaria Notariale ◽  
Adriana Basile ◽  
Elena Montana ◽  
Nunzia Colonna Romano ◽  
Maria Grazia Cacciapuoti ◽  
...  
Keyword(s):  
Bactericidal Activity ◽  
Mytilus Galloprovincialis ◽  
Bacterial Species ◽  
Enterobacter Aerogenes ◽  
Sperm Chromatin ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Intermediate Group

The major acid-soluble protein components of the mussel Mytilus galloprovincialis sperm chromatin consist of the protamine-like proteins PL-II, PL-III and PL-IV, an intermediate group of sperm nuclear basic proteins between histones and protamines. The aim of this study was to investigate the bactericidal activity of these proteins since, to date, there are reports on bactericidal activity of protamines and histones, but not on protamine-like proteins. We tested the bactericidal activity of these proteins against Gram-positive bacteria: Enterococcus faecalis and two different strains of Staphylococcus aureus, as well as Gram-negative bacteria: Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa, Salmonella typhmurium, Enterobacter aerogenes, Enterobacter cloacae, and Escherichia coli. Clinical isolates of the same bacterial species were also used to compare their sensitivity to these proteins. The results show that Mytilus galloprovincialis protamine-like proteins exhibited bactericidal activity against all bacterial strains tested with different minimum bactericidal concentration values, ranging from 15.7 to 250 µg/mL. Furthermore, these proteins were active against some bacterial strains tested that are resistant to conventional antibiotics. These proteins showed very low toxicity as judged by red blood cell lysis and viability MTT assays and seem to act both at the membrane level and within the bacterial cell. We also tested the bactericidal activity of the product obtained from an in vitro model of gastrointestinal digestion of protamine-like proteins on a Gram-positive and a Gram-negative strain, and obtained the same results with respect to undigested protamine-like proteins on the Gram-positive bacterium. These results provide the first evidence of bactericidal activity of protamine-like-proteins.

scholarly journals Effective Small Molecule Antibacterials from a Novel Anti-Protein Secretion Screen

2021 ◽  
Vol 9 (3) ◽  
pp. 592
Author(s):  
Mohamed Belal Hamed ◽  
Ewa Burchacka ◽  
Liselotte Angus ◽  
Arnaud Marchand ◽  
Jozefien De Geyter ◽  
...  
Keyword(s):  
Protein Secretion ◽  
Small Molecule ◽  
Bacterial Resistance ◽  
Bacterial Species ◽  
Attractive Potential ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
Gram Positive Bacteria

The increasing problem of bacterial resistance to antibiotics underscores the urgent need for new antibacterials. Protein export pathways are attractive potential targets. The Sec pathway is essential for bacterial viability and includes components that are absent from eukaryotes. Here, we used a new high-throughput in vivo screen based on the secretion and activity of alkaline phosphatase (PhoA), a Sec-dependent secreted enzyme that becomes active in the periplasm. The assay was optimized for a luminescence-based substrate and was used to screen a ~240K small molecule compound library. After hit confirmation and analoging, 14 HTS secretion inhibitors (HSI), belonging to eight structural classes, were identified with IC50 < 60 µM. The inhibitors were evaluated as antibacterials against 19 Gram-negative and Gram-positive bacterial species (including those from the WHO’s top pathogens list). Seven of them—HSI#6, 9; HSI#1, 5, 10; and HSI#12, 14—representing three structural families, were bacteriocidal. HSI#6 was the most potent hit against 13 species of both Gram-negative and Gram-positive bacteria with IC50 of 0.4 to 8.7 μM. HSI#1, 5, 9 and 10 inhibited the viability of Gram-positive bacteria with IC50 ~6.9–77.8 μM. HSI#9, 12, and 14 inhibited the viability of E. coli strains with IC50 < 65 μM. Moreover, HSI#1, 5 and 10 inhibited the viability of an E. coli strain missing TolC to improve permeability with IC50 4 to 14 μM, indicating their inability to penetrate the outer membrane. The antimicrobial activity was not related to the inhibition of the SecA component of the translocase in vitro, and hence, HSI molecules may target new unknown components that directly or indirectly affect protein secretion. The results provided proof of the principle that the new broad HTS approach can yield attractive nanomolar inhibitors that have potential as new starting compounds for optimization to derive potential antibiotics.

scholarly journals Rosuvastatin as forthcoming antibiotic or as adjuvant additive agent: In vitro novel antibacterial study

2018 ◽  
Vol 10 (03) ◽  
pp. 271-275 ◽  
Author(s):  
Hayder M. Al-Kuraishy ◽  
Ali I. Al-Gareeb ◽  
Ali K. Al-Buhadily
Keyword(s):  
Antibacterial Activity ◽  
Pathogenic Bacteria ◽  
Inhibitory Concentration ◽  
Cholesterol Biosynthesis ◽  
Lipid Lowering ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli

ABSTRACT INTRODUCTION: Rosuvastatin is a lipid-lowering agent that inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase leading to a reduction of cholesterol biosynthesis. Many studies have shown an association between statins use and the reduction of sepsis. The aim of the present study was to evaluate the in vitro combined antibacterial activity of rosuvastatin and cefixime. MATERIALS AND METHODS: Five pathogenic bacteria isolates (Gram positive and Gram negative) were used for testing the antibacterial activity of rosuvastatin alone and in combination with cefixime. Results: Rosuvastatin mainly inhibited Klebsiella pneumoniae and Escherichia coli where it caused zones of inhibition of (17.9 ± 0.6 mm) and (16.9 ± 0.3 mm), respectively; however, it moderately inhibited the growth of Staphylococcus epidermidis (12.9 ± 0.2 mm) and Staphylococcus aureus (12.76 ± 0.2) and produced less inhibition for Pseudomonas aeruginosa growth where it led to a zone of inhibition equal to (9.1 ± 0.5 mm). Minimal inhibitory concentration (μg/mL) of rosuvastatin was high compared to cefixime. Fractional inhibitory concentration (FIC) of rosuvastatin was low for E. coli and K. pneumoniae compared to the other types of bacterial strains. Rosuvastatin exhibited additive effects with cefixime against E. coli and K. pneumoniae. ΣFIC index was 0.536 and 0.734 for E. coli and K. pneumoniae, respectively. Conclusions: Rosuvastatin has a significant antibacterial activity against both Gram-negative and Gram-positive bacteria with a potential additive effect when used in combination with cefixime.

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