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 Design, Synthesis and Evaluation of Schiff’s Bases of 4-Chloro-3-coumarin aldehyde as Antimicrobial Agents

2009 ◽  
Vol 6 (3) ◽  
pp. 759-762 ◽  
Author(s):  
Shriram Bairagi ◽  
Ashok Bhosale ◽  
Meenakshi N. Deodhar
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Design Synthesis ◽  
Gram Negative ◽  
H Nmr ◽  
Nmr Data ◽  
Bacteria And Fungi

4-Chloro-2-oxo-2H-chromene-3-carbaldehyde(2)was reacted with different anilines in rectified spirit as solvent to yield a series of the title compoundsi.e. 4-chloro-3-((substituted-phenylimino) methyl)-2H-chromen-2-one(3a-i). These compounds were charaterised on the basis of their spectral (IR,1H NMR) data and evaluated for antimicrobial activityin vitroagainst gram positive and gram negative bacteria and fungi. Compound3Cwas found to be most active with an MIC of 15 μg /mL against all the tested organisms.

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 The In Vitro Antimicrobial Effects of Lavandula angustifolia Essential Oil in Combination with Conventional Antimicrobial Agents

2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Stephanie de Rapper ◽  
Alvaro Viljoen ◽  
Sandy van Vuuren
Keyword(s):  
Antimicrobial Activity ◽  
Essential Oil ◽  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Antimicrobial Effect ◽  
Antimicrobial Activities ◽  
Lavandula Angustifolia ◽  
Gram Negative ◽  
Stock Solutions

The paper focuses on the in vitro antimicrobial activity of Lavandula angustifolia Mill. (lavender) essential oil in combination with four commercial antimicrobial agents. Stock solutions of chloramphenicol, ciprofloxacin, nystatin, and fusidic acid were tested in combination with L. angustifolia essential oil. The antimicrobial activities of the combinations were investigated against the Gram-positive bacterial strain Staphylococcus aureus (ATCC 6538) and Gram-negative Pseudomonas aeruginosa (ATCC 27858) and Candida albicans (ATCC 10231) was selected to represent the yeasts. The antimicrobial effect was performed using the minimum inhibitory concentration (MIC) microdilution assay. Isobolograms were constructed for varying ratios. The most prominent interaction was noted when L. angustifolia essential oil was combined with chloramphenicol and tested against the pathogen P. aeruginosa (ΣFIC of 0.29). Lavendula angustifolia essential oil was shown in most cases to interact synergistically with conventional antimicrobials when combined in ratios where higher volumes of L. angustifolia essential oil were incorporated into the combination.

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 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.

New Insights Towards 1,4-Benzodiazepines from Curcumin. Design, Synthesis and Antimicrobial Activities

2020 ◽  
Vol 16 (8) ◽  
pp. 1112-1123
Author(s):  
Othman Hamed ◽  
Oswa Fares ◽  
Shaima Taleeb ◽  
Ghaleb Adwan ◽  
Haythem Saadeh ◽  
...  
Keyword(s):  
Biological Activities ◽  
Antimicrobial Activities ◽  
High Potency ◽  
Step Method ◽  
Gram Positive ◽  
Design Synthesis ◽  
Gram Negative ◽  
E Coli ◽  
Gram Positive Bacteria

Background: Curcumin is a safe, versatile natural product with unlimited number of biological activities and a precursor for various heterocyclic compounds. Objective: The present study was aimed to the development of a curcumin based antimicrobial reagent with high potency against gram-positive and gram-negative bacteria. Methods: Herein we report a simple and convenient one step method for synthesizing a series of 1,4-benzodiazepines via condensation cyclization reaction between curcumin and various 1,2- phenylenediamine in refluxed ethanol. Results: A series of new 1,4-benzodiazepins were synthesized and their structures were supported by FT-IR, 1H NMR, 13C NMR, and mass spectral analysis. Synthesized 1,4-benzodiazepins were evaluated for their in vitro antimicrobial activity against gram positive (S. aureus and S. epidermidis) and gram negative (E. coli and P. aeruginosa) bacteria. They exhibited low to high potency against the tested organisms. In particular, dichlorinated 1,4-benzodiazepine 9 exhibited a remarkable potency against the gram-positive bacteria S. aureus (MIC: 3.125 μg mL-1, MBC: 12 μg mL-1). It showed a higher potency than most of the tested reference drugs. Compound 9 showed the medium activity against E. coli. Genotoxic study revealed that, benzodiazepines 9 attacked the DNA of E. coli strains and damaged it. The potency of compound 9, could be attributed to the multiple chlorine atoms present on the aromatic ring. Conclusion: Some of the synthesized curcumin based benzodiazepines showed excellent potency against gram positive bacteria. These benzodiazepines could be a great candidate as a future antimicrobial agent.

scholarly journals 169 Susceptibility of several species of gram-negative and gram-positive bacteria to organic acids and their derivatives

2019 ◽  
Vol 97 (Supplement_2) ◽  
pp. 96-97
Author(s):  
Lauren Kovanda ◽  
Xunde Li ◽  
Wen Zhang ◽  
Xiaohong Wei ◽  
Jia Luo ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Organic Acids ◽  
Formic Acid ◽  
Butyric Acid ◽  
Sodium Formate ◽  
Valeric Acid ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative

Abstract The objective of this experiment was to determine the in vitro antimicrobial activity of several organic acids and their derivatives against gram-positive (G+) and gram-negative (G-) bacteria. Monopropionin, monovalerin, monolaurin, and sodium formate were tested at 10 to 12 concentrations from 0.001 to 2.50 mg/L; monobutyrin was tested at 16 concentrations from 0.001 to 5.00 mg/L; butyric acid and valeric acid were tested at 8 concentrations from 0.001 to 0.35 mg/L; while formic acid was tested at 8 concentrations from 0.001 to 1.00 mg/L. The tested bacteria included G- bacteria (Escherichia coli, Salmonella typhimurium, and Campylobacter jejuni) and G+ bacteria (Enterococcus faecalis, Clostridia perfringens, Streptococcus pneumonia, and Streptococcus suis). Antimicrobial activity of tested compounds was expressed as minimum inhibitory concentration (MIC) that prevented growth of tested bacteria in treated culture broth. Butyric acid, valeric acid, and formic acid at highest tested concentrations inhibited the growth of all bacterial strains. The MICs of the three acids varied among bacterial strains with lowest MIC of 0.05–0.10 mg/L on two strains of Campylobacter. Sodium formate at highest tested concentrations did not inhibit the growth of E. coli, S. typhimurium, and E. faecalis but the compound inhibited the growth of other tested bacteria with MIC values from 0.20 to 1.88 mg/L. The MIC values of monovalerin, monolaurin, and monobutyrin ranged between 0.001 and 1.50 mg/L on all bacterial strains with the exception that monobutyrin did not inhibit C. jejuni (ATCC 33560) growth at the highest concentration tested (5.0 mg/L). Monopropionin at tested concentrations did not inhibit the growth of all tested bacteria with the exception of 1.13 mg/L as MIC on C. perfringens (ATCC 12915). The MIC tests indicate that all organic acids and their derivatives, except monopropionin, tested in this experiment exhibited strong antimicrobial effects in vitro against tested bacterial strains.

scholarly journals Synthesis and Evaluation of Some Coumarin Containing Potential Antimicrobial Agents

2012 ◽  
Vol 9 (4) ◽  
pp. 2493-2500
Author(s):  
Sayali D. Kudale ◽  
Meenakshi N. Deodhar
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Gram Negative Bacteria ◽  
Schiff’S Bases ◽  
Gram Positive ◽  
Gram Negative ◽  
H Nmr ◽  
Nmr Data ◽  
Bacteria And Fungi

A series of the Schiff’s bases incorporating coumarin and chalcone moeities, 3-(4-(4-(substituted phenyl)prop-1-ene-3-one) phenylimino) methyl)-4-chloro-2h-chromen-2-one 4(a-g) were synthesized as potential antimicrobial agents. These compounds were characterized on the basis of their spectral (IR,1H NMR) data and evaluated for antimicrobial activity in vitro against gram positive and gram negative bacteria and fungi. Compound 4b was found to be most active with an MIC of 20 µg/mL against all the tested organisms.

scholarly journals In Vitro Antimicrobial Activities of Organic Acids and Their Derivatives on Several Species of Gram-Negative and Gram-Positive Bacteria

Molecules ◽  
2019 ◽  
Vol 24 (20) ◽  
pp. 3770 ◽  
Author(s):  
Lauren Kovanda ◽  
Wen Zhang ◽  
Xiaohong Wei ◽  
Jia Luo ◽  
Xixi Wu ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Streptococcus Pneumoniae ◽  
Organic Acids ◽  
Enterococcus Faecalis ◽  
Sodium Formate ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
Gram Negative

The objective of this study was to determine the in vitro antimicrobial activity of several organic acids and their derivatives against Gram-positive (G+) and Gram-negative (G−) bacteria. Butyric acid, valeric acid, monopropionin, monobutyrin, monovalerin, monolaurin, sodium formate, and ProPhorce—a mixture of sodium formate and formic acid (40:60 w/v)—were tested at 8 to 16 concentrations from 10 to 50,000 mg/L. The tested bacteria included G− bacteria (Escherichia coli, Salmonella enterica Typhimurium, and Campylobacter jejuni) and G+ bacteria (Enterococcus faecalis, Clostridium perfringens, Streptococcus pneumoniae, and Streptococcus suis). Antimicrobial activity was expressed as minimum inhibitory concentration (MIC) of tested compounds that prevented growth of tested bacteria in treated culture broth. The MICs of butyric acid, valeric acid, and ProPhorce varied among bacterial strains with the lowest MIC of 500–1000 mg/L on two strains of Campylobacter. Sodium formate at highest tested concentrations (20,000 mg/L) did not inhibit the growth of Escherichia coli, Salmonella Typhimurium, and Enterococcus faecalis, but sodium formate inhibited the growth of other tested bacteria with MIC values from 2000 to 18,800 mg/L. The MIC values of monovalerin, monolaurin, and monobutyrin ranged from 2500 to 15,000 mg/L in the majority of bacterial strains. Monopropionin did not inhibit the growth of all tested bacteria, with the exception that the MIC of monopropionin was 11,300 mg/L on Clostridia perfringens. Monolaurin strongly inhibited G+ bacteria, with the MIC value of 10 mg/L against Streptococcus pneumoniae. The MIC tests indicated that organic acids and their derivatives exhibit promising antimicrobial effects in vitro against G− and G+ bacteria that are resistant to antimicrobial drugs. The acid forms had stronger in vitro antimicrobial activities than ester forms, except that the medium chain fatty acid ester monolaurin exhibited strong inhibitory effects on G+ bacteria.

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