scholarly journals Polyhalonitrobutadienes as Versatile Building Blocks for the Biotargeted Synthesis of Substituted N-Heterocyclic Compounds

Molecules ◽  
2020 ◽  
Vol 25 (12) ◽  
pp. 2863 ◽  
Author(s):  
Viktor A. Zapol’skii ◽  
Ursula Bilitewski ◽  
Sören R. Kupiec ◽  
Isabell Ramming ◽  
Dieter E. Kaufmann
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Heterocyclic Compounds ◽  
Nitrogen Heterocycles ◽  
Building Blocks ◽  
Antibacterial Activities ◽  
Synthetic Approach ◽  
Selective Synthesis ◽  
Ic50 Values ◽  
Thiophene Derivatives

Substituted nitrogen heterocycles are structural key units in many important pharmaceuticals. A new synthetic approach towards heterocyclic compounds displaying antibacterial activity against Staphylococcus aureus or cytotoxic activity has been developed. The selective synthesis of a series of 64 new N-heterocycles from the three nitrobutadienes 2-nitroperchloro-1,3-butadiene, 4-bromotetrachloro-2-nitro-1,3-butadiene and (Z)-1,1,4-trichloro-2,4-dinitrobuta-1,3-diene proved feasible. Their reactions with N-, O- and S-nucleophiles provide rapid access to push-pull substituted benzoxazolines, benzimidazolines, imidazolidines, thiazolidinones, pyrazoles, pyrimidines, pyridopyrimidines, benzoquinolines, isothiazoles, dihydroisoxazoles, and thiophenes with unique substitution patterns. Antibacterial activities of 64 synthesized compounds were examined. Additionally, seven compounds (thiazolidinone, nitropyrimidine, indole, pyridopyrimidine, and thiophene derivatives) exhibited a significant cytotoxicity with IC50-values from 1.05 to 20.1 µM. In conclusion, it was demonstrated that polyhalonitrobutadienes have an interesting potential as structural backbones for a variety of highly functionalized, pharmaceutically active heterocycles.

scholarly journals Synthesis and Antibacterial Activity of New Spiro[thiadiazoline-(pyrazolo[3,4-d]pyrimidine)] Derivatives

2015 ◽  
Vol 2015 ◽  
pp. 1-6 ◽  
Author(s):  
Mohammed El Fal ◽  
Youssef Ramli ◽  
Abdelfettah Zerzouf ◽  
Ahmed Talbaoui ◽  
Youssef Bakri ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Spectroscopic Data ◽  
Heterocyclic Compounds ◽  
Dipolar Cycloaddition ◽  
Bacterial Strains ◽  
Pyrimidine Derivatives ◽  
H Nmr ◽  
Biological Interest ◽  
Mic Value

New heterocyclic compounds spiroderivatives of allopurinol of biological interest were prepared from allopurinol via thionation and 1,3-dipolar cycloaddition and were produced in high to excellent yields. These compounds were characterized on the basis of spectral and spectroscopic data (1H NMR,13C, IR, and MS). The antibacterial activity of the synthesized products was studied using bacterial strains:Staphylococcus aureus,Enterococcus faecalis,Escherichia coli, andPseudomonas aeruginosa. Compounds having an ethyl group showed the best activity with MIC value of 31.25 µg/mL againstStaphylococcus aureusandStreptococcus fasciens.

scholarly journals Synthesis and antimicrobial activities of novel n-substituted 8-(1-alkyl/alkylsulphonyl/alkoxycarbonyl-benzimidazol-2-ylmethoxy)-5-chloroquinolines

2011 ◽  
Vol 76 (9) ◽  
pp. 1199-1206 ◽  
Author(s):  
Raju Chaudhari ◽  
Sahebrao Rindhe
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Nitrogen Heterocycles ◽  
Antimicrobial Activities ◽  
Mass Spectral Data ◽  
Antifungal Activities ◽  
Mass Spectral ◽  
Electrophilic Reagents ◽  
Almost All ◽  
And Staphylococcus Aureus

Herein the synthesis of a series of novel 8-(1- alkyl/alkylsulphonyl/alkoxycarbonyl-benzimidazol-2-ylmethoxy)-5- chloroquinoline derivatives is reported. These derivatives were prepared by the condensation of o-phenylenediamine with [(5-chloroquinolin-8- yl)oxy]acetic acid, followed by substitution at nitrogen with different electrophilic reagents in presence of an appropriate base to give a series of nitrogen heterocycles containing the benzimidazole and quinoline nuclei. The structures of the compounds were confirmed based on 1H-NMR, 13CNMR, IR and mass spectral data. Almost all the compounds exhibited promising antibacterial activity against Salmonella typhimurium and Staphylococcus aureus. Some of the compounds showed good antifungal activities against Aspergillus niger but the antifungal activities against Candida albicans were disappointing.

scholarly journals ISOLATION AND CHARACTERIZATION OF ACTINOMYCETES FROM SOIL OF AD-DAWADMI, SAUDI ARABIA AND SCREENING THEIR ANTIBACTERIAL ACTIVITIES

2017 ◽  
Vol 9 (10) ◽  
pp. 276 ◽  
Author(s):  
Gouse Basha Sheik ◽  
Muazzam Sheriff Maqbul ◽  
Gokul Shankar S. ◽  
Ranjith M S
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Antibacterial Activities ◽  
Soil Samples ◽  
Streptomyces Sp ◽  
Crude Extracts ◽  
Test Organisms ◽  
Inhibition Zones

Objective: To isolate and characterize novel actinomycetes and to evaluate their antibacterial activity against drug-resistant pathogenic bacteriaMethods: In the present study, 19 soil samples were collected from different localities of Ad-Dawadmi, Saudi Arabia. Actinomycetes were isolated from these samples using serial dilution and plating method on Actinomycetes isolation agar supplemented with nalidixic acid and actidione to inhibit bacteria and fungi. Crude extracts of potential actinomycetes were produced by submerged fermentation. The antimicrobial activity of crude extracts of actinomycetes was tested against different bacteria using the agar well diffusion method. Characterization of the isolates was done by morphological, physiological and biochemical methods.Results: A total of 9 (47%) isolates of actinomycetes were isolated from 19 different soil samples tested. Among them, 4 (44%) isolates confirmed as Streptomyces sp. showed potential antimicrobial activity against one or more test organisms. Crude extracts were made from these 4 actinomycetes isolates(DOM1, DOM3, DP3, DP4)and tested for their antibacterial activities against 4 different clinical bacterial strains (Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Enterococcus). Crude extract from DP3 isolate showed highest antibacterial activity against all the four test organisms (28 mm, 21 mm, 20 mm and 18 mm) respectively and DP4 showed lowest antibacterial activity against all the four test organisms (14 mm, 12 mm, 0 mm, 6 mm) respectively. The highest zone of inhibition was shown by DP3 against Staphylococcus aureus (28 mm) and Escherichia coli was resistant for DP4. Most of the Inhibition zones produced by crude extracts showed significant differences when compared with control, tested against test organisms (P<0.05). Inhibition zones produced by DP3 and DOM1 against Staphylococcus aureus were 28 mm and 23 mm, respectively which were strong active when compared with control Ciprofloxacin (18 mm).Conclusion: Further studies for purification of bioactive metabolites and molecular characterization analysis of isolated Streptomyces sp. are in progress which would be helpful in discovering novel compounds of commercial value.

scholarly journals Optical characterization and concentration-dependent antibacterial activity of silver nanoparticles (AgNPs) using aqueous Melastoma malabathricum extract against Staphylococcus aureus

2020 ◽  
Vol 11 (4) ◽  
pp. 5382-5387
Author(s):  
Irshad Ul Haq Bhat ◽  
Maisarah Binti Alias
Keyword(s):  
Staphylococcus Aureus ◽  
Silver Nanoparticles ◽  
Antibacterial Activity ◽  
Functional Groups ◽  
Diffusion Method ◽  
Synthetic Approach ◽  
Potential Candidate ◽  
X Ray ◽  
Melastoma Malabathricum ◽  
Resonance Band

The approach towards green synthetic methods has been enormously encouraged to synthesise nanoparticles for various uses. In this study, the one-pot synthetic method was adapted to synthesise silver nanoparticles (AgNPs) using Melastoma malabathricum (M. malabathricum) aqueous extract. The formation of AgNPs was confirmed by observing the results obtained by optical characterisation methods. The plasma resonance band along with shoulder at 375 nm and 595 nm, respectively, in Uv-Visible spectra supported the conversion of silver (Ag) to AgNPs reduced by functional groups present in the plant extract. The size of AgNPs was 31 nm and cubic in shape as confirmed by X-ray diffractometry (XRD) using Scherer equation. X-Ray Fluorescence (XRF) results also confirmed the presence of silver. The FTIR characterisation confirmed the presence of reducing functional groups. The antibacterial activity of AgNPs against Staphylococcus aureus (S. aureus) was carried out by disc diffusion method with increasing concentration of AgNPs, and enhanced inhibition zone was observed. The AgNPs obtained can be further explored against different bacterial strains and can a potential candidate as an antibacterial agent using the green synthetic approach.

scholarly journals Antibacterial and Cytotoxic Activities of the Sesquiterpene Lactones Cnicin and Onopordopicrin

2011 ◽  
Vol 6 (2) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Sandra M. Bach ◽  
Mario A. Fortuna ◽  
Rodgoun Attarian ◽  
Juliana T. de Trimarco ◽  
César A. N. Catalán ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Sesquiterpene Lactones ◽  
Antibacterial Activities ◽  
Chloroform Extract ◽  
Cytotoxic Activities ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
High Cytotoxicity

The antimicrobial and cytotoxic activities of chloroform extracts from the weeds Centaurea tweediei and C. diffusa, and the main sesquiterpene lactones isolated from these species, onopordopicrin and cnicin, respectively, were assayed. Results show that the chloroform extracts from both Centaurea species possess antibacterial activities against a panel of Gram-positive and Gram-negative bacteria. Remarkable antibacterial activity against methicillin-resistant Staphylococcus aureus was also measured. Both the extracts and the purified sesquiterpene lactones show high cytotoxicity against human-derived macrophages. Despite this cytotoxicity, C. diffusa chloroform extract and cnicin are attractive candidates for evaluation as antibiotics in topical preparations against skin-associated pathogens.

scholarly journals Chemical composition, antibacterial activity and related mechanism of valonia and shell from Quercus variabilis Blume (Fagaceae) against Salmonella paratyphi a and Staphylococcus aureus

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Dan Zhou ◽  
Ze-Hua Liu ◽  
Dong-Mei Wang ◽  
Deng-Wu Li ◽  
Li-Na Yang ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Chemical Composition ◽  
Antibacterial Activities ◽  
Diffusion Method ◽  
Antibacterial Mechanism ◽  
Natural Antimicrobials ◽  
Butanol Fraction ◽  
Quercus Variabilis ◽  
Crude Extracts

Abstract Background Plant secondary metabolites and phytochemicals that exhibit strong bioactivities have potential to be developed as safe and efficient natural antimicrobials against food contamination and addressing antimicrobial resistance caused by the overuse of chemical synthetic preservative. In this study, the chemical composition, antibacterial activities and related mechanism of the extracts of the valonia and the shell of Quercus variabilis Blume were studied to determine its potential as a safe and efficient natural antimicrobial. Methods The phenolic compositions of valonia and shell extracts were determined by folin-ciocalteau colourimetric method, sodium borohydride/chloranil-based assay and the aluminium chloride method and then further identified by the reverse-phase HPLC analysis. The antibacterial activities of valonia and shell extracts were evaluated by the agar disk diffusion method and agar dilution method. The related antibacterial mechanism was explored successively by the membrane of pathogens effect, phosphorous metabolism, whole-cell proteins and the microbial morphology under scanning electron microscopy. Results The n-butanol fraction and water fraction of valonia along with n-butanol fraction of the shell contains enrich phenolics including ellagic acid, theophylline, caffeic acid and tannin acid. The n-butanol fraction and ethanol crude extracts of valonia exhibited strong antibacterial activities against Salmonella paratyphi A (S. paratyphi A) and Staphylococcus aureus (S. aureus) with the DIZ values ranged from 10.89 ± 0.12 to 15.92 ± 0.44, which were greater than that of the Punica granatum (DIZ: 10.22 ± 0.18 and 10.30 ± 0.21). The MIC values of the n-butanol fraction and ethanol crude extracts of valonia against S. paratyphi A and S. aureus were 1.25 mg/ml and 0.625 mg/ml. The related antibacterial mechanism of n-butanol fraction and ethanol crude extracts of valonia may be attributed to their strong impact on membrane permeability and cellular metabolism. Those extracts exhibited strong antibacterial activity according to inhibit the synthesis of bacterial proteins and seriously change morphological structure of bacterial cells. Conclusions The n-butanol fraction and ethanol crude extracts of valonia had reasonably good antibacterial activities against S. paratyphi A and S. aureus. This study suggests possible application of valonia and shell as natural antimicrobials or preservatives for food and medical application.

Antibacterial Activity of Amine-Functionalized Zeolite NaY against Staphylococcus aureus ATCC6538 and Escherichia coli ATCC11229

2015 ◽  
Vol 761 ◽  
pp. 402-406 ◽  
Author(s):  
Siti Aishah Mohd Hanim ◽  
Nik Ahmad Nizam Nik Malek ◽  
Zaharah Ibrahim ◽  
Mashitah Mad Salim ◽  
Nur Isti'anah Ramli ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Inhibition Zone ◽  
Antibacterial Activities ◽  
Gram Positive ◽  
Gram Negative ◽  
Zeolite Nay ◽  
Amine Functionalized ◽  
Diffusion Technique

The antibacterial activity of functionalized zeolite NaY (CBV100) with different concentrations of 3-aminopropyltriethoxysilane (APTES) (0.01, 0.05, 0.20 and 0.40 M) was studied against Staphylococcus aureus ATCC 6538 (Gram positive) and Escherichia coli ATCC 11229 (Gram negative) through disc diffusion technique (DDT). The characterization of functionalized zeolite NaY with fourier transform infrared (FTIR) spectroscopy indicated the attachment of APTES on zeolite NaY. Through DDT, the inhibition zone of functionalized zeolite NaY increased proportionally to the amount of the amine-functional group attached onto zeolite NaY. Functionalized zeolite NaY showed higher antibacterial activity against Gram-positive compared to Gram-negative bacteria. It can be concluded from this study that amine-functionalized zeolite NaY shows evidence of antibacterial activities.

Preparation, Characterization and Antibacterial Activity of Chitosan Schiffbases

2011 ◽  
Vol 287-290 ◽  
pp. 1947-1951 ◽  
Author(s):  
Jing Xian Xu ◽  
Ye Ting Lin ◽  
Qiang Lin ◽  
Wen Yuan ◽  
Xue Qiong Yin ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Schiff Bases ◽  
Optical Density ◽  
Elemental Analysis ◽  
Antibacterial Activities ◽  
Cp Mas Nmr ◽  
And Staphylococcus Aureus ◽  
Better Than

Two Schiff bases of chitosan (CTS) were synthesized from 4-methoxylbenzylaldehyde (CH3O-CTS) and 4-methylbenzylaldehyde(CH3-CTS). The Schiff bases were characterized by FTIR, DSC-TGA, solid13C CP-Mas NMR, and elemental analysis. Antibacterial activities of the Schiff bases against Escherichia coli and Staphylococcus aureus were measured by the optical density method. The antibacterial activity of the Schiff bases is better than that of the original CTS. The IC50of CH3O-CTS and CH3-CTS againstEscherichia coliis respectively 40.3 ppm and 43 ppm, which being 38.5 ppm and 39.5 ppm against Staphylococcus aureus, lower than IC50of chitosan, being 59.5 ppm and 52 ppm againstEscherichia coliand Staphylococcus aureus, respectively.

Synthesis and Antibacterial Activities of N-Phenylpyrazolines from Veratraldehyde

2017 ◽  
Vol 901 ◽  
pp. 124-132
Author(s):  
Artania Adnin Tri Suma ◽  
Tutik Dwi Wahyuningsih ◽  
Deni Pranowo
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Bacillus Subtilis ◽  
Bacillus Cereus ◽  
Shigella Flexneri ◽  
Inhibition Zone ◽  
Antibacterial Activities ◽  
Diffusion Method ◽  
Agar Well Diffusion Method

Some novel N-phenylpyrazolines were synthesized and investigated for their antibacterial activitiy. Chalcones 2-4 which were prepared from acetophenone and veratraldehyde derivatives were reacted with phenylhydrazine to give N-phenylpyrazolines 5-7. All of the synthesized compounds were characterized using FTIR, GC-MS, and NMR spectrometers. Further, antibacterial activity of N-phenylpyrazolines were evaluated by agar well-diffusion method against Staphylococcus aureus, Bacillus cereus, Bacillus subtilis, Escherichia coli, and Shigella flexneri. The highest activity (highest inhibition zone) of compound 5 was 2.6 mm (at 1000 ppm) against B. subtillis, compound 6 was 7.25 mm (at 1000 ppm) against S. aureus, and compound 7 was 6.75 mm (at 500 ppm) against S. aureus. The results indicated that compound 6 and 7 exhibited promising antibacterial activity.

scholarly journals SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF SOME 1,4- AND 1,4,5-SUBSTITUTED-1H-1,2,3TRIAZOLES IN RELATION TO THE STAPHYLOCOCCUS AUREUS STRAIN

2018 ◽  
Vol 62 (3) ◽  
pp. 293-297 ◽  
Author(s):  
A. V. Zuraev ◽  
A. V. Lishai ◽  
Yu. V. Grigoriev ◽  
O. A. Ivashkevich
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Catalytic System ◽  
Bactericidal Activity ◽  
Cycloaddition Reaction ◽  
Antibacterial Activities ◽  
Aureus Strain ◽  
Derivatives Of

A number of 1,4- and 1,4,5-triazoles have been synthesized using a modified catalytic system for the Huisgen [3+2] cycloaddition reaction. The bactericidal activity of the synthesized compounds has been studied. The synthesized derivatives of 1H-1,2,3-triazoles have demonstrated higher antibacterial activities in relation to the pathogen Staphylococcus aureus strain which can be comparable with the clinically used antibiotic “Cefotaxime”.

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