Synthesis, structural analysis, antimicrobial evaluation and synergistic studies of imidazo[1,2-a]pyrimidine chalcogenides

RSC Advances ◽  
2016 ◽  
Vol 6 (115) ◽  
pp. 114224-114234 ◽  
Author(s):  
Nidhi Sharma ◽  
Sanjeev Kumar ◽  
Indresh K. Maurya ◽  
K. K. Bhasin ◽  
Ajay Verma ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Structural Analysis ◽  
Synergistic Effects ◽  
Antimicrobial Evaluation

Synthesis and structural analysis of novel imidazo[1,2-a]pyrimidine chalcogenides exhibiting effective antimicrobial activity and synergistic effects with known antibiotics have been reported.

scholarly journals Green ultrasound-assisted three-component click synthesis of novel 1H-1,2,3-triazole carrying benzothiazoles and fluorinated-1,2,4-triazole conjugates and their antimicrobial evaluation

2017 ◽  
Vol 67 (3) ◽  
pp. 309-324 ◽  
Author(s):  
Nadjet Rezki ◽  
Mohamed Reda Aouad
Keyword(s):  
Antimicrobial Activity ◽  
Cycloaddition Reaction ◽  
Dipolar Cycloaddition ◽  
Terminal Alkynes ◽  
One Pot ◽  
Alkyl Aryl ◽  
Antimicrobial Evaluation ◽  
Ultrasound Assisted ◽  
Click Synthesis

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.

scholarly journals Extraction and Characterization of Silver Nitrate Modified Biopolymer and its Antimicrobial Mode of Action

2021 ◽  
pp. 50-62
Author(s):  
Jeje O. Ayorinde ◽  
Osula J. Eghosa
Keyword(s):  
Antimicrobial Activity ◽  
Silver Nitrate ◽  
Mode Of Action ◽  
Proximate Analysis ◽  
Klebsiella Pneumonia ◽  
Crab Shell ◽  
Agno3 Solution ◽  
Antimicrobial Evaluation ◽  
Ft Ir ◽  
Crab Shell Waste

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.

scholarly journals Development of Novel Thin Polycaprolactone (PCL)/Clay Nanocomposite Films with Antimicrobial Activity Promoted by the Study of Mechanical, Thermal, and Surface Properties

Polymers ◽  
2021 ◽  
Vol 13 (18) ◽  
pp. 3193
Author(s):  
Sylva Holešová ◽  
Karla Čech Čech Barabaszová ◽  
Marianna Hundáková ◽  
Michaela Ščuková ◽  
Kamila Hrabovská ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Surface Properties ◽  
Food Packaging ◽  
Synergistic Effects ◽  
Nanocomposite Films ◽  
Mechanical Resistance ◽  
X Ray Diffraction ◽  
Microbial Strains ◽  
And Storage ◽  
Structure Properties

Infection with pathogenic microorganisms is of great concern in many areas, especially in healthcare, but also in food packaging and storage, or in water purification systems. Antimicrobial polymer nanocomposites have gained great popularity in these areas. Therefore, this study focused on new approaches to develop thin antimicrobial films based on biodegradable polycaprolactone (PCL) with clay mineral natural vermiculite as a carrier for antimicrobial compounds, where the active organic antimicrobial component is antifungal ciclopirox olamine (CPX). For possible synergistic effects, a sample in combination with the inorganic antimicrobial active ingredient zinc oxide was also prepared. The structures of all the prepared samples were studied by X-ray diffraction, FTIR analysis and, predominantly, by SEM. The very different structure properties of the prepared nanofillers had a fundamental influence on the final structural arrangement of thin PCL nanocomposite films as well as on their mechanical, thermal, and surface properties. As sample PCL/ZnOVER_CPX possessed the best results for antimicrobial activity against examined microbial strains, the synergic effect of CPX and ZnO combination on antimicrobial activity was proved, but on the other hand, its mechanical resistance was the lowest.

scholarly journals Synthesis, Molecular Docking and Antimicrobial Evaluation of Some Benzothiazoles

2021 ◽  
Author(s):  
Smita J. Pawar ◽  
Amol Kale ◽  
Priya Zori ◽  
Rahul Dorugade
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Property ◽  
Docking Study ◽  
Gram Negative Bacteria ◽  
Zone Of Inhibition ◽  
E Coli ◽  
Good Antibacterial Activity ◽  
Comparable Activity ◽  
Antimicrobial Evaluation ◽  
Bacteria And Fungi

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.

Synergistic Effects of Essential Oils of Ammoides verticillata and Satureja candidissima Against Many Pathogenic Microorganisms

2020 ◽  
Vol 18 (1) ◽  
pp. 72-78 ◽  
Author(s):  
Fatima Benyoucef ◽  
Mohammed El Amine Dib ◽  
Boufeldja Tabti ◽  
Arrar Zoheir ◽  
Jean Costa ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Essential Oil ◽  
Essential Oils ◽  
Synergistic Effects ◽  
Lactobacillus Rhamnosus ◽  
Salmonella Typhi ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
Gram Negative ◽  
Ammoides Verticillata

Background: Antibiotic resistance is today one of the most serious threats to global health, food security and development. Due to the growing number of infections, treatment becomes more difficult, if not impossible, because of the loss of antibiotic efficacy. Objective: In the present investigation, the chemical composition of essential oils of Ammoides verticillata and Satureja candidissima and their synergistic effects on antimicrobial activities were investigated. Methods: The chemical composition of the essential oil was analyzed by Gas Chromatography (GC) and Gas Chromatography-Mass Spectroscopy (GC/MS). The antimicrobial activity of the essential oils was investigated using dilution-agar method against nine bacterial strains three Gram-negative Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853) and Salmonella typhi (ATCC 14028), and six Gram-positive: Staphylococcus aureus (ATCC 43300,) Clostridium sporogenes (ATCC 19404), Bacillus subtilis (ATCC 6633), Enterococcus faecalis (ATCC 7314), Lactobacillus rhamnosus (ATCC 53103) and Bacillus cereus (ATCC 14579). Results: The essential oil of A. verticillata was characterized principally by carvacrol (44,3%), Limonene (19,3%) and p-cymene (19,2%). The constituents identified of S. candidissima essential oil were principally oxygenated monoterpenes represented by pulegone (70,4%). The essential oil of A. verticillata had a good antimicrobial activity against four bacterial strains (Escherichia coli, Salmonella typhi, Lactobacillus rhamnosus and Bacillus cereus) with MIC and MBC values between 0.2-0.4 µl/ml and 0.2-6.2 µl/ml, respectively. While, S. candidissima essential oil had moderate antimicrobial activities against all strains with MIC and MBC values between 1.5-6.2 µl/ml and 6.2-12.5 µl/ml, respectively. The results of antimicrobial activity of essential oils blend presented higher antimicrobial activity against all tested bacteria with MIC and MBC values between 0.3-1.5 µl/ml and 0.4-6.2 µl/ml, respectively. Conclusion: The essential oils blend presented high antimicrobial activity compared to virgin oils. This activity can be due to the association of active compounds such as carvacrol and pulegone. These findings provide a new source of drugs that may help in therapy to lead to the development of a new treatment based on a combination of these essential oils against gram-negative and gram-positive bacteria that continue to pose a threat to public health.

ANTIMICROBIAL ACTIVITY OF COPPER KAOLINITE AND SURFACTANT MODIFIED COPPER KAOLINITE AGAINST GRAM POSITIVE AND GRAM NEGATIVE BACTERIA

2016 ◽  
Vol 78 (3-2) ◽  
Author(s):  
Nor Syafawani Sarah Md Saad ◽  
Nik Ahmad Nizam Nik Malek ◽  
Chun Shiong Chong
Keyword(s):  
Antimicrobial Activity ◽  
Synergistic Effects ◽  
Wide Spectrum ◽  
Copper Nitrate ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
X Ray ◽  
Gram Positive Bacteria ◽  
Diffusion Technique

The aim of this research was to determine the antimicrobial activity of kaolinite modified with antimicrobial compounds against Gram positive and Gram negative bacteria. Copper kaolinite (Cu-kaolinite) was prepared by loading raw kaolinite with copper nitrate trihydrate (CuNO3) while surfactant modified Cu-kaolinite (SM-Cu-kaolinite) was prepared by adding cationic surfactants hexadecyltrimethyl ammonium (HDTMA) on Cu-Kaolinite. Samples was characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM) and energy dispersive X-ray (EDX) analyzer. The antimicrobial activity of the samples was tested against Gram negative bacteria (Escherichia coli ATCC 11229 and Pseudomonas aeruginosa ATCC 15442), and Gram positive bacteria (Staphylococcus aureus ATCC 6538 and Enterococcus faecalis ATCC 29212) through disc diffusion technique (DDT) and minimum inhibition concentration (MIC). The results showed that the antimicrobial activity of Cu-kaolinite increased after modified with HDTMA due to the synergistic effects of Cu ions and HDTMA molecules on the kaolinite. The antimicrobial activity for surfactant modified Cu-kaolinite was greater for Gram positive bacteria compared to Gram negative bacteria. In conclusion, the attachment of HDTMA on Cu-kaolinite contributed to the enhanced antimicrobial activity against wide spectrum of bacteria (Gram positive and Gram negative bacteria).

scholarly journals Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1339 ◽  
Author(s):  
Islam H. El Azab ◽  
Nadia A.A. Elkanzi
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Positive Control ◽  
Design Synthesis ◽  
Aspergillus Brasiliensis ◽  
In Vitro Investigation ◽  
Bacillus Subtilis Atcc ◽  
Antimicrobial Evaluation

A series of 34 new pyrimido[2,1-c][1,2,4]triazine-3,4-diones were synthesized and fully characterized using IR, NMR, MS, and microanalytical analysis. In vitro investigation of 12 compounds of this series revealed promising antimicrobial activity of the conjugates 15a and 15f–j that were tagged with electron-withdrawing groups, with sensitivities ranging from 77% to as high as 100% of the positive control. The investigation of antimicrobial activity included Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 6535, Pseudomonas aeruginosa ATCC 27853, and Escherichia coli ATCC 8739 (EC), and fungal strains Candida albicans ATCC 10231 and Aspergillus brasiliensis ATCC 16404.

Structural analysis and antimicrobial activity of 2[1H]-pyrimidinethione/selenone derivatives

2017 ◽  
Vol 1142 ◽  
pp. 261-266 ◽  
Author(s):  
Ewa Żesławska ◽  
Izabela Korona-Głowniak ◽  
Małgorzata Szczesio ◽  
Andrzej Olczak ◽  
Alicja Żylewska ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Structural Analysis

Synergistic effects of chitosan–guanidine complexes on enhancing antimicrobial activity and wet-strength of paper

2010 ◽  
Vol 101 (14) ◽  
pp. 5693-5700 ◽  
Author(s):  
Shengling Sun ◽  
Qiaozhi An ◽  
Xu Li ◽  
Liying Qian ◽  
Beihai He ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Synergistic Effects ◽  
Wet Strength

scholarly journals CHITOSAN NANOPARTICLES AS DRUG DELIVERY SYSTEM FOR CEPHALEXIN AND ITS ANTIMICROBIAL ACTIVITY AGAINST MULTIIDRUG RESISTENT BACTERIA

2019 ◽  
pp. 14-27 ◽  
Author(s):  
Mona Elassal ◽  
Nagwan El-Manofy
Keyword(s):  
Antimicrobial Activity ◽  
Electron Microscope ◽  
Mammalian Cells ◽  
Synergistic Effects ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Clinical Isolates ◽  
Antibiofilm Activity ◽  
Diffusion Kinetic

Objective: The evolution of antimicrobial resistance is a universal obstacle that necessities the innovation of more effective and safe antimicrobial alternatives with synergistic properties. The purpose of this study was to investigate the possible improvement of cephalexin antimicrobial treatments by loading into chitosan-based nanoparticles, then evaluate their antibacterial and antibiofilm activities as well as determination of its cytotoxicity. Methods: Chitosan nanoparticles (CSNPs) were prepared by ionic gelation method. Parameters were studied to optimize the particle size of CSNPs including pH, stirring rate, homogenization and ultra-sonication time. Size was measured by transmission electron microscope (TEM) and Zeta sizer, morphology seen by scanning electron microscope (SEM). Entrapment efficiency, drug loading and drug content were calculated. Stability of both plain and loaded chitosan Nano-carriers, Drug release and Kinetics also compatibilities were studied. Antimicrobial activity of CSNPs and cephalexin loaded CSNPs were evaluated against 4 Gram-positive and 4 Gram-negative standard and clinical isolates by microdilution method, also assessment of antibiofilm activity of both formulas was investigated against two biofilm producers clinical isolates by tube assay in addition to determination of their cytotoxicity by MTT(3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. Results: Chitosan nanoparticles and its loaded antibiotics proved compatible combination with small Zeta size, suitable Zeta potential, maximum EE% and drug-loading capacity, sustained controlled release properties followed diffusion kinetic model and six month stability studies. Cephalexin loaded CSNPs showed better antimicrobial activity than plain CSNPs. Synergistic effects were found against S. aureus (ATCC 25923), B. subtilis (ATCC 9372), S. epidermidis, E. faecalis, P. aeruginosa (ATCC 29853) in addition to two carbapenem resistant isolates k. pneumoniae and E. coli. Also cephalexin loaded CSNPs exhibited antibiofilm activity against E. faecalis clinical isolate. Even though, cephalexin loaded CSNPs exhibited significant antibacterial activity, it showed less toxicity against mammalian cells, it had IC50 equal to 231.893 and did not exhibit any cytotoxicity against the WI-38 fibroblast cells at concentration 23.4 µg/ml. Conclusion: Cephalexin loaded CSNPs possessed good stability and sustained release effect in addition to its antimicrobial, antibiofilm activities and reduced cytotoxicity.

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