scholarly journals Synthesis of New Oxindoles and Determination of Their Antibacterial Properties

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Pablo E. Romo ◽  
Braulio Insuasty ◽  
Rodrigo Abonia ◽  
María del Pilar Crespo ◽  
Jairo Quiroga

A versatile method for the synthesis of new oxindoles was developed by the reaction between substituted isatins and 5-aminopyrazoles. The reaction was carried out at room temperature in ethanol using p-toluenesulfonic acid as the catalyst. The products were obtained with acceptable to excellent yields (44–96%). Structures of the new compounds were unambiguously established by spectroscopic and analytical techniques. The antibacterial activity was determined by microdilution assays. Compounds 3b, 3e, and 3g showed antistaphylococcal activity, particularly compound 3e displayed a potent activity against the vancomycin intermediate Staphylococcus aureus (VISA). Compounds 3i, 3j, and 3o inhibited Neisseria gonorrhoeae growth.

Author(s):  
Pari Tamri ◽  
Shabnam Pourmoslemi ◽  
Shirin Moradkhani ◽  
Sahar Foroughinia

Scrophularia. striata from Scrophulariacea family has been used in Iranian folk medicine for the treatment of infectious diseases. In this study we evaluated the synergistic effect of S. striata   hydroalcoholic extract (SSE) and commercially available antibiotics against P. aeroginosa and Methicillin- resistant Staphylococcus aureus (MRSA). The resazurin-based microdilution method was used to determine the minimum inhibitory concentration (MIC) values of plan extract and standard antibiotics. The interaction between standard antibiotics and SSE was evaluated by using checkerboard method. The results of this study revealed that SSE enhance the antibacterial activity of antibiotics. The combination of SSE and Vancomycin had synergistic to additive effects against MRSA.  SSE in combination with Gentamicin had synergistic to additive effects against P. aeruginosa. The interaction between Ceftazidime and SSE was additive against P. aeruginosa.  The best result was the synergistic effect between SSE and Piperacillin-Tazobactam against P. aeruginosa. In conclusion the results of this research indicated that S. striata has the potential to enhance the antibacterial activity of antibiotics and could be a source to the designing new compounds with synergistic effect in combination with standard antibiotics.


2020 ◽  
Vol 35 (2) ◽  
pp. 274-286
Author(s):  
Claudia M Alonzo-de la Rosa ◽  
Francesco Copes ◽  
Pascale Chevallier ◽  
Jonnathan G Santillán-Benitez ◽  
Georgina Carbajal-de la Torre ◽  
...  

Polyethylene glycol has been widely investigated for wound healing and dressing applications. Despite its advantages (i.e. great biocompatibility), polyethylene glycol lacks antibacterial activity. For this reason, semi-interpenetrated polymeric networks were prepared by combining a chemically cross-linked polyethylene glycol network with chitosan. The aim of this work was to identify the best amount of chitosan able to improve the antibacterial properties against Staphylococcus aureus. Briefly, the networks were synthesized by a sequential method, adding chitosan in different proportion to the polyethylene glycol. The antibacterial activity was tested following the MGA 0100 of the Pharmacopeia of the United States of Mexico. Fourier-transform infrared with attenuated total reflection spectroscopy, scanning electron microscopy and swelling behavior PBS at 37° C and room temperature were also performed to characterize the polymeric networks. The results showed that PC-2% was able to inhibit the bacterial growth of Staphylococcus aureus even more than Fosfomycin antibiotic. The networks showed cylindrical pores of different sizes (50–100 µm). The maximum swelling of all the networks was achieved in PBS at 37°C (>315%). Free hemoglobin and hemolysis assays were also evaluated to know the compatibility with erythrocytes. Human dermal fibroblasts were used to evaluate direct cytotoxicity. Therefore, the produced gels exerted interesting antibacterial activity and showed good biocompatibility properties.


Materials ◽  
2020 ◽  
Vol 13 (7) ◽  
pp. 1782
Author(s):  
Amir M. Ashrafi ◽  
Pavel Kopel ◽  
Lukas Richtera

The electrochemical redox behavior of three trinuclear Ni(II) complexes [Ni3(abb)3(H2O)3(µ-ttc)](ClO4)3 (1), [Ni3(tebb)3(H2O)3(µ-ttc)](ClO4)3·H2O (2), and [Ni3(pmdien)3(µ-ttc)](ClO4)3 (3), where abb = 1-(1H-benzimidazol-2-yl)-N-(1H-benzimidazol-2-ylmethyl)methan-amine, ttcH3 = trithiocyanuric acid, tebb = 2-[2-[2-(1H-benzimidazol-2-yl)ethylsulfanyl]ethyl]-1H-benzimidazole, and pmdien = N,N,N′,N″,N″-pentamethyldiethylenetriamine is reported. Cyclic voltammetry (CV) was applied for the study of the electrochemical behavior of these compounds. The results confirmed the presence of ttc and nickel in oxidation state +2 in the synthesized complexes. Moreover, the antibacterial properties and cytotoxic activity of complex 3 was investigated. All the complexes show antibacterial activity against Staphylococcus aureus and Escherichia coli to different extents. The cytotoxic activity of complex 3 and ttcNa3 were studied on G-361, HOS, K-562, and MCF7 cancer cell lines. It was found out that complex 3 possesses the cytotoxic activity against the tested cell lines, whereas ttcNa3 did not show any cytotoxic activity.


2014 ◽  
Vol 875-877 ◽  
pp. 87-90 ◽  
Author(s):  
Chutimon Satirapipathkul ◽  
Tanakan Chatdum

The film-forming potential of isolate of seed polysaccharide fromCassia fistulawas investigated. Increasing the glycerol concentration in the film increased elongation at break, film solubility and water vapor permeability but decreased tensile strength (TS). The film impregnated with the acetone extract ofAtractylodes lanceawas assessed for inhibition ofEscherichia coliandStaphylococcus aureus. The obtained results showed that the films exhibited antibacterial activity against both bacterial strains. Disc-diffusion assay revealed that the film resulted in a larger inhibition zone around the film onStaphylococcus aureusthan it did onEscherichia coliat the same extract concentrations (0.1 to 0.9 wt %). It can be seen that the film has satisfactory physical and antibacterial properties.


2020 ◽  
Vol 840 ◽  
pp. 293-299
Author(s):  
Poedji Loekitowati Hariani ◽  
Muryati Muryati ◽  
Muhammad Said ◽  
Salni Salni

Nano-hydroxyapatite was synthesized by coprecipitation method and tested its antibacterial properties. Nano-hydroxyapatite was synthesized using CaO precursors from snakehead (Channa striata) fish bones and (NH4)2HPO4. The synthesis was carried out with temperature variations of 30, 60, 80, and 100 °C. Antibacterial activity was determined using two types of bacteria, namely gram-positive and gram-negative. The XRD spectra show that the highest peak is hydroxyapatite synthesized at a temperature of 100 °C. Hydroxyapatite produced from various synthesis temperatures has the size of nanoparticles in the range 37.32-49.27 nm. The nano-hydroxyapatite functional groups are characterized using FTIR, the analysis indicate the presence of OH, CO32‒ and PO43‒. The molar ratio Ca/P is obtained of 1.71 approaching theoretical hydroxyapatite of 1.67. The resulted nano-hydroxyapatite has significant antibacterial properties to Escherichia coli and Staphylococcus aureus.


2007 ◽  
Vol 51 (4) ◽  
pp. 1559-1562 ◽  
Author(s):  
Aldona L. Baltch ◽  
William J. Ritz ◽  
Lawrence H. Bopp ◽  
Phyllis B. Michelsen ◽  
Raymond P. Smith

ABSTRACT We investigated the antistaphylococcal activity of daptomycin, vancomycin, oxacillin, gentamicin, and rifampin in human monocyte-derived macrophages. Compared with vancomycin and oxacillin, daptomycin had the most rapid and greatest antibacterial activity, but that of oxacillin was most sustained. The combination of daptomycin, gentamicin, and rifampin was most effective intracellularly, while daptomycin plus gentamicin and the three-drug combination were most effective extracellularly, completely eliminating viable Staphylococcus aureus.


1947 ◽  
Vol 134 (877) ◽  
pp. 538-543 ◽  

A series of basic derivatives of cholane and norcholane has been examined for bacteriostatic activity against the Gram-positive Staphylococcus aureus and Lactobacillus helveticus and the Gram-negative Bacillus lactis aerogenes . The basic derivatives, in general, were more highly bacteriostatic against the Gram-positive organisms than against the Gram-negative. Of the compounds studied, the highest antibacterial activity was shown by 3:7:12-trihydroxy-23-guanido-norcholane hydrochloride. No relationship was apparent between the lowering of the surface tension of the medium induced by the compounds and their bacteriostatic activity.


2017 ◽  
Vol 95 (9) ◽  
pp. 927-934 ◽  
Author(s):  
Elena Fuentes-Paniagua ◽  
José M. Hernández-Ros ◽  
Juan Soliveri ◽  
José L. Copa-Patiño ◽  
Rafael Gómez ◽  
...  

Strategies to synthesize a cationic carbosilane dendron containing the antibiotic penicillin V potassium salt (PenVK) at the focal point are discussed. The preparation of such a compound requires the use of systems with no donor atoms such as N or S in their framework, because their presence favours the rupture of the penicillin β-lactam ring. The antibacterial activity of the new dendron containing ammonium groups, at the periphery, and the PenV moiety, at the focal point, against gram-positive Staphylococcus aureus strains was evaluated. These results were compared with those obtained for free PenVK, a related cationic dendron without a penicillin moiety at the focal point, and also compared with an equimolar mixture of this last dendron with free PenV. The data obtained indicate that, on one hand, the conjugation or interaction of PenV with cationic dendrons reduces its activity in comparison with free PenVK. On the other hand, the penicillin dendron is able to release the antibiotic in the presence of esterease, due to the breaking of the ester bond in this derivative.


2014 ◽  
Vol 1052 ◽  
pp. 327-331 ◽  
Author(s):  
Jian Rong Wang ◽  
Ya Li Liu ◽  
Bin Liu ◽  
Yan Ping Wu

A novel method was used to make palygorskite supported nano-silver powder at room temperature. XRD result showed the presence of silver in the final product. TEM investigation revealed that nano-sliver particles of 6-10 nm in diameter were successfully attached on surface of palygorskite fiber. FTIR was also used to clarify the formation mechanism of our method. The antibacterial effect of palygorskite supported nano-silver powder was investigated. Palygorskite supported nano-silver powder had good antibacterial activity on standard Escherichia coli and Staphylococcus aureus.


2017 ◽  
pp. 63-70 ◽  
Author(s):  
Наталья (Natal'ja) Александровна (Aleksandrovna) Коваленко (Kovalenko) ◽  
Галина (Galina) Николаевна (Nikolaevna) Супиченко (Supichenko) ◽  
Татьяна (Tat'jana) Игоревна (Igorevna) Ахрамович (Ahramovich) ◽  
Анна (Anna) Геннадьевна (Gennad'evna) Шутова (Shutova) ◽  
Виктор (Viktor) Николаевич (Nikolaevich) Леонтьев (Leontiev)

The essential oil obtained by hydrodistillation method from plants of three varieties Agastache aurantiaca, cultivated on the Republic of Belarus were investigated. Some morphobiometric parameters of plants 'Tango', 'Apricot Sprite' and 'Fragrant Delight' and oil yields were determined. Using the technique of gas-liquid chromatography essential oil components were identified and determined. The main components of the essential oil from 'Tango' and 'Fragrant Delight' plants were menton (~ 53 and ~ 65 v/v % respectively) and pulegon (~ 36 and ~ 25 v/v % respectively). The samples of 'Apricot' Sprite' essential oil were rich in isomentone (~ 46 v/v %) and pulegon (~ 41 v/v %). All tested essential oils contained (+)-menton and (+)-pulegon enantiomeric forms only. The antibacterial activity of dimethylsulfoxide and ethanolic essential oil solutions against Staphylococcus aureus, Salmonella alony, Bacillus subtilis, Clostridium sp., Escherichia coli Hfr H, Pseudomonas aeruginosa was proved. Ethanol solutions of essential oils at the concentrations 0.001–0.1 v/v % had significant bactericidal activity. A correlation between the composition of the essential oil and their antibacterial properties was established.


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