scholarly journals Synthesis, Characterization and Antibacterial Activity of Carbamate Derivatives of Isatin

2018 ◽  
Vol 34 (4) ◽  
pp. 2026-2030 ◽  
Author(s):  
Sarrah Sattar Jabbar

In search of novel antibacterial agent, a series of new isatin derivatives (3a-d) have been synthesized by condensation isatin (2,3-indolinendione) with piperidine (hexahydropyridine), hydrazine hydrate and Boc-amino acids respectively. Compounds synthesized have been characterized by IR spectroscopy and elemental analysis. In addition, the in vitro antibacterial properties have been tested against E. coli, P. aeruginosa, and Bacillus cereus, S. aureus by employing the well diffusion technique. A majority of the synthesized compounds were showing good antibacterial activity and from comparisons of the compounds, compound 3d has been determined to be the most active compound.

2021 ◽  
Vol 6 (3) ◽  
pp. 189-195
Author(s):  
Hary Widjajanti ◽  
Christina Vivid Handayani ◽  
Elisa Nurnawati

The antibiotic resistance of phatogenic bacteria has become a serious health problem and has encouraged the search for novel and effective antimicrobial metabolites. Meanwhile, endophytic fungi have great potential as a natural source for antimicrobial agents. The endophytic fungi that live in plant tissue produces secondary metabolites which potentially act as an antibacterial compound. The isolation of fungi for antibacterial sources reduces the large amount of plant as a source of antibacterial agents. Hence, this study aims to obtain endophytic fungi isolates from Paederia foetida L. that are capable of producing secondary metabolites as antibacterial, carry out in vitro tests to verify the antibacterial properties of secondary metabolites of the Paederia foetida L. endophytic fungi, and identify the potential of Paederia foetida L. endophytic fungi in producing antibacterial compounds. The antibacterial activity was tested against Escherichia coli ATCC8739 and Staphylococcus aureus ATCC6538 while seven isolates of endophytic fungi that potentially produced antibacterial were obtained from Sembukan (P. foetida L.). The results showed that antibacterial activities of SL1, SL4 and SL6 secondary metabolites against S. aureus ATCC6538 and E. coli ATCC8739 were moderate to strong activities. Furthermore, the Minimum Inhibition Concentration (MIC) of secondary metabolites extract of SL1 against S. aureus ATCC6538 value was 250 ????g/mL while the values of MIC extract of SL4 against S. aureus ATCC6538 and E. coli ATCC8739 were 125 ????g/mL and 250 ????g/mL respectively and MIC extract of SL6 against E. coli ATCC8739 value was 125 ????g/mL. The secondary metabolites extract of SL1 isolate were alkaloid and tannin, SL4 were phenolic and alkaloid while SL6 isolate were alkaloid and terpenoid. Hence, endophytic fungi SL1 isolate was identified as Fusarium sp., SL4 as Dematophora sp., and SL6 isolate as Acremonium sp.


Author(s):  
Sri Atun ◽  
Sri Handayani ◽  
Melia Aliffiana ◽  
Hajar Nur Afifah ◽  
Anna Rakhmawati

The antibacterial activity of three Cupressaceae plants (Thujaoccidentalis,ThujaorientalisandChamaecyparisobtusa) was tested against three bacteria using the agar diffusion method. The ether and ethylacetate fraction of crude methanol extract from the three plants showed potent antibacterial activity against the tested microorganisms. The result showed that Staphylococcus aureus revealed the most sensitivity among the tested bacteria. Thujaoccidentalisether fraction and Thujaorientalis hexane fraction exhibited the highest antibacterial activity against Staphylococcus aureus. E. coli was shown the highest MIC values compared to the other two tested bacteria, which indicates the lowest antibacterial activity against the bacterium. This study promises an interesting future for designing a potentially active antibacterial agent from the three Cupressaceae plants.


Nanomaterials ◽  
2021 ◽  
Vol 11 (6) ◽  
pp. 1621
Author(s):  
Yuelong Xu ◽  
Hongxia Wang ◽  
Min Zhang ◽  
Jianhao Zhang ◽  
Wenjing Yan

d-cysteine (d-cys) has been demonstrated to possess an extraordinary antibacterial activity because of its unique steric configuration. However, inefficient antibacterial properties seriously hinder its wide applications. Here, cysteine-functionalized gold nanoparticles (d-/l-Au NPs) were prepared by loading d-/l-cysteine on the surface of gold nanoparticles for the effective inhibition of Escherichia coli (E. coli) in vitro and in vivo, and the effects on the intestinal microflora in mice were explored during the treatment of E. coli infection in the gut. We found that the antibacterial activity of d-/l-Au NPs was more than 2–3 times higher than pure d-cysteine, l-cysteine and Au NPs. Compared with l-Au NPs, d-Au NPs showed the stronger antibacterial activity, which was related to its unique steric configuration. Chiral Au NPs showed stronger destructive effects on cell membrane compared to other groups, which further leads to the leakage of the cytoplasm and bacterial cell death. The in vivo antibacterial experiment illustrated that d-Au NPs displayed impressive antibacterial activity in the treatment of E. coli-infected mice comparable to kanamycin, whereas they could not affect the balance of intestinal microflora. This work is of great significance in the development of an effective chiral antibacterial agent.


2016 ◽  
Vol 64 (3) ◽  
Author(s):  
Nelson Méndez Álvarez ◽  
Alberto Angulo Ortíz ◽  
Orfa Contreras Martínez

Bacterial resistance is a growing health problem worldwide that has serious economic and social impacts, compromising public health, and the therapeutic action of current antibiotics. Therefore, the search for new compounds with antimicrobial properties is relevant in modern studies, particularly against bacteria of clinical interest. In the present study, in vitro antibacterial activity of the ethanol extract and essential oil of Curcuma longa (Zingiberaceae) was evaluated against nosocomial bacteria, using the microdilution method. Escherichia coli strains, Pseudomonas aeruginosa, Klebsiella pneumoniae, Proteus sp. were used, Salmonella sp. and Bacillus sp., isolated from nosocomial infections in a hospital in the city of Monteria and reference strains of S. aureus ATCC 43300, S. aureus ATCC 29213, S. aureus ATCC 25923, P. aeruginosa ATCC 27853, E. coli ATCC 25922 and K. pneumonia ATCC 700603. The ethanol extract antibacterial profile was more efficient at higher concentrations (1 000 ppm), obtaining significant percentages of reduction of more than 50 % against K. pneumoniae ATCC 700603 and a clinical isolate of E. coli; while compared to Bacillus clinical isolate, was more active than the essential oil. For the rest of microorganisms, the reduction percentages obtained at a concentration of 1 000 ppm varied between 17 and 42 % with ethanolic extract, and 8 to 43 % with essential oil. At concentrations of 100 and 500 ppm antibacterial activity of the extracts was lower. The results indicated that the ethanolic extract and essential oil of C. longa rhizomes have active compounds with antibacterial properties that could be used in future research as a therapeutic alternative for the treatment of infections caused by nosocomial pathogens.


2011 ◽  
Vol 8 (1) ◽  
pp. 240-244 ◽  
Author(s):  
Anoop K. Pathak ◽  
Viney Chawla ◽  
Shailendra K. Saraf

A new series of 1,3-pyrimidine derivatives (3a-f) have been synthesized by reacting 2,4,6-Trichloropyrimidine with nucleophilic reagents 2-amino-6-fluorobenzothiazole (1) in the presence of acetone. The (4,6- dichloro-pyrimidin-2-yl)-amine (2) so produced was then reacted to two moles of phenylthiourea derivatives to yield title compounds (3a-f). The structural assessment of the compounds (3a-f) was made on the basis of spectral data. The synthesized compounds were screened for theirin vitrogrowth inhibiting activity against different strains of bacteriaviz.,B. subtilis, E. coli, P. aeruginosaandS. aureususing agar diffusion technique. Compounds3cand3fexhibited highest antibacterial activity.


Author(s):  
Hemanth K Sudheer Kumar ◽  
Parameshwar H

Objective: The present study envisage a series of sparfloxacin derivatives were synthesized (Q1-Q10) with added derivatives such as aminomethyl benzenesulfenyl, methyl (methylamino)benzenesulfenyl, amino methyl benzoyl chloride, nitromethyl benzoyl chloride, dimethyl phenylamino, methoxymethyl phenylamino, dimethyl oxopyrazol, methyl dioxopyrrolidine, methyl oxopyrrolidine, and N-Boc amino methyl methylpyrrolidine through N-Piperzinyl linkage.Methods: All the newly synthesized compounds were characterized by infrared,1H nuclear magnetic resonance, mass spectrometry, and elemental analysis technique, screened for docking stimulation to find out binding modes of synthesized derivatives with 3FV5 and 3IMW, and evaluated for in vitro antimicrobial activity.Results: From this study, it was found that the compound Q5 showed good antibacterial activity against Gram-positive (Staphylococcus aureus) and compound Q4 showed good antibacterial activity against Gram-negative (Escherichia coli) in comparison with standard drugs (ciprofloxacin and sparfloxacin). The zone of inhibition and minimum inhibitory concentrations studies performed to synthesized compounds. The correlation between experimental data (minimum inhibitory concentrations) and docking score suggests that penetration for docking simulation is good to mild in reproducing experimental orientation of these synthesized compounds.Conclusion: The analogs of sparfloxacin are suggested to be potent inhibitors with sufficient scope for further exploration.


Author(s):  
Seema U. Shinde ◽  
Nikita D. Gidde ◽  
Jamir. A. Tamboli

Bacterial skin infections are the most prevalent among individuals, necessitating immediate treatment as well as ongoing care to preserve healthy skin. Because some herbal plant extracts have antibacterial properties, the goal of this research is to make an antibacterial poly herbal bath soap using curcuma longa[Turmeric] and Organum Vulgare [Oregano The antibacterial activity of prepared soap was evaluated against staphylococcus aureus, E. coli, and Aspergillus Niger using the agar well diffusion technique. The developed Polyherbal formulation had a good antibacterial activity, and it was analysed for several physicochemical parameters and whether it has good characteristics. Plants are easily obtainable, and their efficacy helps manufacturers in achieving cost-effective outcomes with few or no side effects.


2021 ◽  
Vol 285 ◽  
pp. 05012
Author(s):  
A. K. Milyuhinа ◽  
L. A. Zabodalova ◽  
U. Kyzdarbek ◽  
I. R. Romazyaeva ◽  
N. Yu. Klyuchko

Rosmarinus officinalis L. is known for its antioxidant and antibacterial properties against a variety of microorganisms. In this work, research has been carried out on pharmacy rosemary. Its antioxidant and antimicrobial properties have been determined. This study showed that the ethanol extract of R. officinalis L. has a pronounced antimicrobial activity against strains of both gram-positive and gram-negative bacteria. The extract also showed good antioxidant activity. Rosemary showed significantly more potent antibacterial activity against E. coli. The diameter of the zone of oppression was 17 mm. Thus, Rosemary Pharmaceutical has demonstrated potential as a dietary supplement due to its stronger antibacterial activity.


2020 ◽  
Vol 8 (6) ◽  
pp. 962
Author(s):  
R.L. McMurray ◽  
M.E.E. Ball ◽  
M.M. Tunney ◽  
N. Corcionivoschi ◽  
C. Situ

The worldwide ethnobotanical use of four investigated plants indicates antibacterial properties. The aim of this study was to screen and determine significant antibacterial activity of four plant extracts in vitro and in a poultry digest model. Using broth microdilution, the concentrations at which four plant extracts inhibited Listeria monocytogenes, Salmonella enteritidis, and Escherichia coli over 24 h was determined. Agrimonia pilosa Ledeb, Iris domestica (L.) Goldblatt and Mabb, Anemone chinensis Bunge, and Smilax glabra Roxb all exhibited a minimum inhibitory concentration (MIC) of 62.5 mg/L and a minimum bactericidal concentration (MBC) of 500 mg/L against one pathogen. A. pilosa Ledeb was the most effective against L. monocytogenes and E. coli with the exception of S. enteritidis, for which A. chinensis Bunge was the most effective. Time–kills of A. pilosa Ledeb and A. chinensis Bunge against L. monocytogenes, E. coli and S. enteritidis incubated in poultry cecum were used to determine bactericidal activity of these plant extracts. A. chinensis Bunge, significantly reduced S. enteritidis by ≥ 99.99% within 6 h. A. pilosa Ledeb exhibited effective significant bactericidal activity within 4 h against L. monocytogenes and E. coli. This paper highlights the potential of these plant extracts to control pathogens commonly found in the poultry gastrointestinal tract.


2020 ◽  
Vol 7 (1) ◽  
pp. 12
Author(s):  
Gabriele Meroni ◽  
Joel F. Soares Filipe ◽  
Piera A. Martino

Silver nanoparticles (AgNPs) are promising alternatives to antibiotics. The aims of this study were to produce AgNPs using two biological methods and determine their antibacterial activity against Pseudomonas aeruginosa and Staphylococcus pseudintermedius. AgNPs were biosynthesized from an infusion of Curcuma longa (turmeric) and the culture supernatant of E. coli. Characterization was achieved by ultraviolet-visible spectroscopy and by Transmission Electron Microscopy (TEM). The antibacterial properties of NPs from C. longa (ClAgNPs) and E. coli (EcAgNPs), alone and in combination with carbenicillin and ampicillin, were investigated through the Kirby-Bauer disk diffusion assay and the minimum inhibitory concentration (MIC). Dimensions of NPs ranged from 11.107 ± 2.705 nm (ClAgNPs) to 27.282 ± 2.68 nm (EcAgNPs). Kirby-Bauer and MIC assays showed great antibacterial abilities for both NPs alone and in combination with antibiotics. EcAgNPs alone showed the most powerful antibacterial activities, resulting in MIC values ranging from 0.438 ± 0.18 µM (P. aeruginosa) to 3.75 ± 3.65 µM (S. pseudintermedius) compared to those of ClAgNPs: 71.8 ± 0 µM (P. aeruginosa) and 143.7 ± 0 µM (S. pseudintermedius). The antibiofilm abilities were strain-dependent, but no statistical differences were found between the two NPs. These results suggest the antibacterial potential of AgNPs for the treatment of infectious diseases.


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