Synthesis, antimicrobial evaluation and molecular modeling of some novel phenothiazine derivatives

RSC Advances ◽  
2015 ◽  
Vol 5 (98) ◽  
pp. 80844-80852 ◽  
Author(s):  
Ahmed A. Fadda ◽  
Ahmed Fekri ◽  
Nesma M. Bayoumy

A novel series of phenothiazine derivatives were synthesized and examined for antimicrobial activity. Most of the newly synthesized compounds exhibited high antimicrobial activity and the results were proven using theoretical data.

2019 ◽  
Vol 10 ◽  
pp. 1864-1872
Author(s):  
Prof. Teodora P. Popova

The effect of ionized aqueous solutions (anolytes and catholyte) in the processing of fruits (cherries, morellos, and strawberries) for decontamination has been tested. Freshly prepared analytes and catholyte without the addition of salts were used, as well as stored for 7 months anolytes, prepared with 0.5% NaCl and a combination of 0.5% NaCl and 0.5% Na2CO3. The anolyte prepared with a combination of 0.5% NaCl and 0.5% Na2CO3, as well as the anolyte obtained with 0.5% NaCl, exhibit high antimicrobial activity against the surface microflora of strawberries, cherries, and sour cherries. They inactivate E. coli for 15 minutes. The other species of the fam. Enterobacteriaceae were also affected to the maximum extent, as is the total number of microorganisms, especially in cherries and sour cherries. Even stored for 7 months, they largely retain their antimicrobial properties. Anolyte and catholyte, obtained without the addition of salts, showed a lower effect on the total number of microorganisms, but had a significant effect on Gram-negative bacteria, and especially with regard to the sanitary indicative E. coli.


MedChemComm ◽  
2019 ◽  
Vol 10 (6) ◽  
pp. 896-900 ◽  
Author(s):  
Takashi Misawa ◽  
Chihiro Goto ◽  
Norihito Shibata ◽  
Motoharu Hirano ◽  
Yutaka Kikuchi ◽  
...  

Amphipathic helical peptideStripeshowed high antimicrobial activity, low hemolytic activity, and low human cell cytotoxicity.


2009 ◽  
Vol 17 (8) ◽  
pp. 3028-3036 ◽  
Author(s):  
Salomão Dória Jorge ◽  
Andrea Masunari ◽  
Carlota Oliveira Rangel-Yagui ◽  
Kerly Fernanda Mesquita Pasqualoto ◽  
Leoberto Costa Tavares

2012 ◽  
Vol 14 (9) ◽  
pp. 2550 ◽  
Author(s):  
Zdenka Marková ◽  
Karolína Šišková ◽  
Jan Filip ◽  
Klára Šafářová ◽  
Robert Prucek ◽  
...  

2017 ◽  
Vol 67 (3) ◽  
pp. 309-324 ◽  
Author(s):  
Nadjet Rezki ◽  
Mohamed Reda Aouad

AbstractThe present study describes an efficient and ecofriendly, ultrasound, one-pot click cycloaddition approach for the construction of a novel series of 1,4-disubstituted-1,2,3-triazoles tethered with fluorinated 1,2,4-triazole-benzothiazole molecular conjugates. It involved three-component condensation of the appropriate bromoacetamide benzothiazole, sodium azide and 4-alkyl/aryl-5-(2-fluorophenyl)-3-(prop-2-ynylthio)-1,2,4-triazoles4a-ethrough a Cu(I)-catalyzed 1,3-dipolar cycloaddition reaction. This approach involvesin situgeneration of azidoacetamide benzothiazole, followed by condensation with terminal alkynes in the presence of CuSO4/Na-ascorbate in aqueous DMSO under both conventional and ultrasound conditions. Some of the designed 1,2,3-triazole conjugates6a-owere recognized for their antimicrobial activity against some bacterial and fungal pathogenic strains.


2009 ◽  
Vol 75 (9) ◽  
pp. 2735-2741 ◽  
Author(s):  
Joseph O. Falkinham ◽  
Thomas E. Wall ◽  
Justin R. Tanner ◽  
Khaled Tawaha ◽  
Feras Q. Alali ◽  
...  

ABSTRACT Anecdotes, both historical and recent, recount the curing of skin infections, including diaper rash, by using red soils from the Hashemite Kingdom of Jordan. Following inoculation of red soils isolated from geographically separate areas of Jordan, Micrococcus luteus and Staphylococcus aureus were rapidly killed. Over the 3-week incubation period, the number of specific types of antibiotic-producing bacteria increased, and high antimicrobial activity (MIC, ∼10 μg/ml) was observed in methanol extracts of the inoculated red soils. Antibiotic-producing microorganisms whose numbers increased during incubation included actinomycetes, Lysobacter spp., and Bacillus spp. The actinomycetes produced actinomycin C2 and actinomycin C3. No myxobacteria or lytic bacteriophages with activity against either M. luteus or S. aureus were detected in either soil before or after inoculation and incubation. Although protozoa and amoebae were detected in the soils, the numbers were low and did not increase over the incubation period. These results suggest that the antibiotic activity of Jordan's red soils is due to the proliferation of antibiotic-producing bacteria.


Author(s):  
Jeje O. Ayorinde ◽  
Osula J. Eghosa

Biopolymer (chitosan) was isolated from crab shell waste through the processes of demineralization, deproteinization, decolourization and deacetylation. The resulting chitosan (CHS) was further treated with silver nitrate (AgNO3) solution at various concentrations (0.5, 1.0 and 1.5 M) in order to enhance the antimicrobial activity of chitosan. The crab shell powder (CSP) and (CHS) were characterized using X-ray Diffractometer (XRD), Fourier Transform Infrared (FT-IR), and Scanning Electron Microscopy coupled with Energy Dispersive Spectroscopy (SEM-EDS). The antimicrobial mode of action of AgNO3 treated chitosan was performed using serial dilution (1:2) technique for minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) and tested against four microorganisms (Escherichia coli, Klebsiella pneumonia, Staphlococcusaureus and Pseudopodium). The result of proximate analysis of CHS and chitin (CHN) showed % crude protein to be 12.24±001 and 20.54±0.03 respectively, % ash was found to be 4.1±0.01 for CHS and 3.80±0.01 for CHN. The FTIR spectra of CHS and CHN showed their characteristic absorption peaks and the diffractograms of CSP and CHS showed CaCO3 to be the major mineral present in the samples. The antimicrobial evaluation revealed that untreated chitosan extract (UCHSE) showed no antimicrobial activity against the four tested microorganisms. The results of MIC and MBC showed that the organisms responded to the antimicrobial agent at different dilution concentration. It was observed that CHS treated with 0.5 M AgNO3 (0.5 SNCHSE) inhibited the growth of E. coli at 1000 µg/mL, S. aureus at 500 µg/mL while it exhibited bactericidal (MBC) activity against all the organisms at 1000 µg/mL.


2014 ◽  
Vol 1 ◽  
Author(s):  
Horta Andre ◽  
Pandeirada Raquel ◽  
Fernandes Lurdes ◽  
Alves Celso ◽  
Pinteus Susete ◽  
...  

2021 ◽  
Author(s):  
Smita J. Pawar ◽  
Amol Kale ◽  
Priya Zori ◽  
Rahul Dorugade

Abstract Abstract The new series of 2-(substituted amino)-N-(6- substituted-1,3-benzothiazol-2yl) acetamide BTC(a-t) has been synthesized by appropriate synthetic route from substituted 2-amino benzothiazole. The synthesized compounds were screened experimentally for its antimicrobial property against gram positive, gram negative bacteria and fungi. Zone of inhibition and minimum inhibitory concentration of compounds was determined against selected bacterial and fungal strains. Compound BTC-j N-(6-methoxy-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide and compound BTC-r N-(6-nitro-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide found to have good antimicrobial potential. The compound BTC-j has shown good antibacterial activity against S. aureus at MIC of 12.5 µg/ml, B. subtilis at MIC of 6.25µg/ml, E. coli at MIC of 3.125µg/ml and P. aeruginosa at MIC of 6.25µg/ml. No statistical difference in antimicrobial activity of standard and test compounds was found indicating test compounds have comparable activity. Further docking study was carried out to check the probable interactions with the selected protein using V-life MDS 3.5 software. (DNA gyrase, PDB: 3G75). The dock score of compounds and antimicrobial activity found to be consistent.


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