Microwave-assisted synthesis and antibacterial activity of derivatives of 3-[1-(4-fluorobenzyl)-1H-indol-3-yl]-5-(4-fluorobenzylthio)-4H-1,2,4-triazol-4-amine

2014 ◽  
Vol 68 (3) ◽  
Author(s):  
Yong-Le Peng ◽  
Xing-Li Liu ◽  
Xiao-Hong Wang ◽  
Zhi-Gang Zhao

AbstractHerein, an excellent method for the synthesis of twelve novel Schiff base derivatives containing indole and triazole assisted by microwave irradiation is reported. Compared with the conventional method, the yields increased from 59–84 % to 85–96 % and the reaction time was reduced from 24–30 h to 4–8 min. Moreover, all series of the newly synthesized Schiff bases were evaluated for their antibacterial activity. The values of minimum inhibitory concentration (MIC) and IC50 indicated that many target compounds possessed excellent antibacterial activity against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, and Bacillus subtilis.

2020 ◽  
Vol 2020 ◽  
pp. 1-6
Author(s):  
Amal Ramzi ◽  
Bouchra Oumokhtar ◽  
Yassine Ez zoubi ◽  
Touria Filali Mouatassem ◽  
Moussa Benboubker ◽  
...  

Background. The microbiological risk of the hospital environment, including inert surfaces, medical devices, and equipment, represents a real problem. Objective. This study is aimed at demonstrating and assessing the antibacterial activity of three synthetic disinfectants classified as quaternary ammoniums on different bacterial strains (Gram-negative and Gram-positive like Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Pseudomonas aeruginosa, Acinetobacter baumannii, and Staphylococcus aureus) isolated from the hospital environment. The reference strains included Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 29213, and Pseudomonas aeruginosa ATCC 27853 used as negative control strains. Method. Three quaternary ammonium disinfectants were tested: DDN9® (0.5%) which contains didecylmethylpolyoxyethylammonium propionate as an active substance, spray (0.4%) containing quaternary ammonium compounds, and Phagosurf ND® (0.4%) with didecyldimethylammonium chloride. Their effect was evaluated using the disk diffusion technique and the broth dilution methods, allowing the Minimum Inhibitory Concentration (MIC) and then the Minimum Bactericidal Concentration (MBC). Result. Only the growth of Gram-positive bacteria and some strains of Gram-negative bacteria were inhibited by the three synthetic disinfectants. NDD9® demonstrated an antibacterial effect only against the Gram-positive strains (S. aureus and S. aureus ATCC 29213) with a MIC of 0.25 mg/ml. The disinfectant spray showed effect against all four strains including E. coli (9), S. aureus, E. coli ATCC 25922, and P. aeruginosa ATCC 27853 with an inhibitory concentration of 4 mg/ml, while the growth of S. aureus ATCC 29213 was inhibited at 2 mg/ml. The third disinfectant, Phagosurf ND®, inhibited only the growth of S. aureus ATCC 29213 at a MIC of 4 mg/ml. Conclusion. This study is the first here in Morocco to evaluate the bacterial activity of products intended for the control of the healthcare environment. The results obtained on the three disinfectants tested reveal an ineffectiveness against some isolated strains from the hospital environment.


2013 ◽  
Vol 2013 ◽  
pp. 1-5
Author(s):  
Anju Goyal ◽  
Sandeep Jain

A series of 1-phenyl-3-(4-(2-ethanoloxy) phenyl)-5-aryl-1H-pyrazoles were synthesized from chalcones, that is, 3-aryl-1-(4-hydroxyphenyl) prop-2-en-1-ones and studied for theirin vitroantibacterial activity. Chalcones1on reaction with phenyl hydrazine in the presence of acetic acid and few drops of hydrochloric acid yielded the corresponding 1-phenyl-3-(4-hydroxyphenyl)-5-aryl-1H-pyrazoles2which on further reaction with 2-chloroethanol furnished the title compounds3. These compounds were characterized by CHN analyses, IR, mass and1H NMR spectral data. All the compounds were evaluated for theirin vitroantibacterial activity against two Gram positive strains (Bacillus subtilisandStaphylococcus aureus) and two Gram negative strains (Escherichia coliandPseudomonas aeruginosa), and their minimum inhibitory concentration (MIC) was determined.


Antibiotics ◽  
2019 ◽  
Vol 8 (1) ◽  
pp. 22
Author(s):  
Ana Carvalho ◽  
Cleciana Cruz ◽  
Cicero Freitas ◽  
José Aguiar ◽  
Paula Nunes ◽  
...  

The present study aimed to determine the chemical profile and to evaluate the antibacterial activity and antibiotic-modulating action of the hexanic Zea mays silk extract in association with aminoglycosides. Standard Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853 strains, as well as multi-resistant Escherichia coli 27, Staphylococcus aureus 35, and Pseudomonas aeruginosa 31 strains, were used in this study. Phytochemical prospection revealed the presence of the following secondary metabolites: tannins, flavones, flavonoids, and xanthones, with the main chemical constituents being identified in plant extracts obtained with apolar organic solvents such as hexane. The extract presented a minimum inhibitory concentration (MIC) ≥1024 μg/mL against all the tested strains. The association of the extract with aminoglycoside antibiotics showed significant synergistic effects against Staphylococcus aureus and Pseudomonas aeruginosa, except for amikacin, which was antagonized by the extract against E. coli. These results indicate the Zea mays silk presents bioactive compounds with antibiotic-modulating properties. However, further research is required to characterize the effects of isolated compounds and determine their potential for drug development.


2009 ◽  
Vol 4 (11) ◽  
pp. 1934578X0900401 ◽  
Author(s):  
Shirley Baldovino ◽  
Janne Rojas ◽  
Luis B. Rojas ◽  
María Lucena ◽  
Alexis Buitrago ◽  
...  

The essential oil from the leaves of Monticalia andicola Turcz., collected in November 2008, was analyzed by GC/MS. A yield of 0.15% oil was obtained by hydrodistillation. Thirty-six components were identified by comparison of their mass spectra with those in the Wiley GC-MS Library data base. The major components were α-pinene (19.6%), β-pinene (10.5%), α-longipinene (6.5%), δ-3-carene (6.2%), cyperene (5.4%) and β-phellandrene (5.2%). The antibacterial activity of the essential oil was evaluated against Gram- positive (Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212) and Gram-negative (Escherichia coli ATCC 25992, Klebsiella pneumoniae ATCC 23357, Pseudomonas aeruginosa ATCC 27853) bacteria, using the disc diffusion agar method. The results showed a broad spectrum of activity with minimal inhibitory concentration (MIC) values ranging from 10 to150 μg/mL.


2018 ◽  
Vol 16 (S1) ◽  
pp. S155-S163 ◽  
Author(s):  
S. Mehalaine ◽  
O. Belfadel ◽  
T. Menasria ◽  
A. Messaili

The present study was carried out to determine, for the first time, the chemical composition and antibacterial activity of essential oils derived from the aerial parts of three aromatic plants Thymus algeriensis Boiss & Reut, Rosmarinus officinalis L., and Salvia officinalis L. growing under semiarid conditions. The essential oils were chemically analyzed and identified by gas chromatography (GC) and GC/ mass spectrometry (GC/MS) and their antimicrobial activity was individually evaluated against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa using both agar disk diffusion and agar dilution methods. The major constituents of Thymus algeriensis essential oil were identified as camphor (13.62%), 1,8-cineol (6.00%), borneol (5.74%), viridiflorol (4.00%), and linalool (3.93%). For Rosmarinus officinalis essential oil, 48 compounds were characterized, of which the main constituents were camphor (17.09%), Z-β-ocimene (10.88%), isoborneol (9.68%), α-bisabolol (7.89%), and borneol (5.11%). While, Salvia officinalis essential oil was characterized by β-thujone (16.44%), followed by viridiflorol (10.93%), camphor (8.99%), 1,8-cineol (8.11%), trans-caryophyllene (5.85%), and α-humulene (4.69%) as the major components. Notably, results from antibacterial screening indicated that Thymus algeriensis and Salvia officinalis essential oils exhibited a strong inhibitory effect against both Escherichia coli and Staphylococcus aureus compared to Rosmarinus officinalis essential oil. Further, less activity was recorded against Pseudomonas aeruginosa for the three tested essential oils.


2018 ◽  
Vol 21 (0) ◽  
Author(s):  
Flávia Cíntia de Oliveira ◽  
Tamara Rezende Marques ◽  
Gustavo Henrique Andrade Machado ◽  
Thaís Cristina Lima de Carvalho ◽  
Aline Aparecida Caetano ◽  
...  

Abstract The phenolic compounds from various extracts of jabuticaba skin powder (JSP) were characterized in this study, and the antibacterial activity assessed. The phenolic compounds were extracted from the JSP using four methods: a) acetone extraction - 1 g JSP: 10 mL 70% acetone, resting for 2 hours; b) aqueous extract - 1 g JSP: 15 mL water, under agitation; c) ethanolic extract - 1 g JSP: 15 mL acidified ethanol, under agitation; and d) methanolic extract - 1 g JSP: 50 mL 50% methanol, under reflux. The antibacterial activity was evaluated by the agar diffusion assay, using Escherichia coli ATCC 11229, Salmonella choleraesuis ATCC 6539, Pseudomonas aeruginosa ATCC 15442, Staphylococcus aureus ATCC 6538 and Listeria monocytogenes ATCC 19117. The ethanolic and methanolic extracts showed the highest levels of phenolic compounds, especially of cyanidin chloride, catechin and epicatechin. The extracts did not inhibit the growth of Escherichia coli and Salmonella choleraesuis, but inhibited 30% of the growth of Pseudomonas aeruginosa with an extract concentration of 250 µg mL-1. Against Staphylococcus aureus and Listeria monocytogenes the highest inhibitory effect observed was 41.8% for the ethanolic extract, followed by 36% inhibition by the methanolic extract, thus revealing the potential of these extracts as possible alternatives for use in the food and/or pharmaceutical industries.


2021 ◽  
Vol 5 (1) ◽  
pp. 1-9
Author(s):  
Antonio Carlos Pereira de Menezes Filho ◽  
Matheus Vinícius Abadia Ventura ◽  
Carlos Frederico de Souza Castro

Tibouchina granulosa is a species that blooms annually in several regions of Brazil. This species is still little explored in terms of phytocompounds in all organs of this plant, especially the floral organ. Flowers of T. granulosa were collected in the municipality of Rio Verde, Goiás, Brazil, in 2021. The hydroethanolic floral extract was prepared by maceration and qualitative phytochemical (colorimetric reactions and salt formation) and antibacterial analyzes performed and the results expressed in millimeters of inhibition at different concentrations in mg mL-1. Several phytochemical classes were observed with positive results, especially for alkaloids, phenolics, oxylates, saponins, carbohydrates and tannins. As for the bacterial assay, potential antibacterial activity was observed for all bacterial strains tested, except for Salmonella serovar Thyphymurium and serovar Enteritidis. Expressive inhibitions were observed for Enterococcus faecalis > Pseudomonas aeruginosa > Staphylococcus aureus and Escherichia coli at the highest concentrations between 100-50 mg mL-1. The floral extract of Tibouchina granulosa showed phytotherapeutic potential with the presence of several phytochemical groups and expressive antibacterial activity.


2018 ◽  
Vol 13 (7) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Subrat Kumar Bhattamisra ◽  
Chew Hui Kuean ◽  
Lee Boon Chieh ◽  
Vivian Lee Yean Yan ◽  
Chin Koh Lee ◽  
...  

The antibacterial activity of geraniol and its effect in combination with ampicillin, amoxicillin and clarithromycin against Staphylococcus aureus, Escherichia coli and Helicobacter pylori was tested. The minimum inhibitory concentrations (MICs) and combinatory effects of geraniol against the bacteria were assessed by using the modified broth microdilution and checkerboard assay, respectively. The combinatory effect is expressed as fractional inhibitory concentration index (FICI). The MIC of geraniol against S. aureus, E. coli and H. pylori was found to be 11200, 5600, and 7325 μg/mL, respectively. A significant synergistic effect was observed with geraniol and ampicillin against S. aureus with FICI in the range 0.19 to 0.32. Geraniol and ampicillin exhibited a partial synergistic effect against E. coli. A similar effect was observed with geraniol and clarithromycin against S. aureus. A partial synergistic effect was observed with clarithromycin and geraniol against H. pylori with the FICI value in the range 0.86 to 0.89. An additive effect was observed with geraniol and amoxicillin combination against H. pylori. However, the amoxicillin and clarithromycin dose was reduced by thirty-two fold when combined with geraniol against H. pylori. The anti- H. pylori effect of geraniol with clarithromycin and amoxicillin could be of potential interest in the treatment of H. pylori infection and associated ulcers in humans. Further, geraniol, in combination with other antibiotics, has substantial therapeutic potential against S. aureus and E.coli infection.


2018 ◽  
Vol 85 (0) ◽  
Author(s):  
Gabriela Silva Moura ◽  
Ivan Júnior de Oliveira ◽  
Lisandro Tomas da Silva Bonome ◽  
Gilmar Franzener

ABSTRACT: Natural products extracted from plants have always played an important role in the discovery of bioactive substances. This work carried out a review of the literature on the bioactive activities of Eugenia uniflora L. (Surinam cherries), as a potential plant in the various uses, be it medicinal, antimicrobial, antioxidant, insecticide and protective. In the literature, studies were found to confirm the antibacterial activity of E. uniflora leaves extract on Streptococcus, Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. The presence of antioxidant compounds as total phenolics, such as anthocyanins and flavonoids, induction in the protection of plants by phytoalexins, as well as insecticidal and anthelmintic effects by the use of the extract of the E. uniflora tree. Although these different potential biotics of E. uniflora have already been reported, further studies are still needed on the use of natural products extracted from E. uniflora for employment for different purposes.


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