scholarly journals Synthesis, Redox Properties and Antibacterial Activity of Hindered Phenols Linked to Heterocycles

Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2370 ◽  
Author(s):  
Vladimir N. Koshelev ◽  
Olga V. Primerova ◽  
Stepan V. Vorobyev ◽  
Ludmila V. Ivanova
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Platinum Electrode ◽  
Redox Properties ◽  
Good Activity ◽  
Pyrimidine Derivatives ◽  
Tert Butyl ◽  
Oxidation Potentials ◽  
Butyl Phenol ◽  
Hindered Phenols

A series of benzotriazole, cyclic amides and pyrimidine derivatives, containing 2,6-di-tert-butyl-phenol fragments, were synthesized. The redox properties of obtained compounds were studied using the cyclic voltammetry on a platinum electrode in acetonitrile. The oxidation potentials of all substances were comparable to those of BHT. The obtained compounds were tested for their antibacterial activity, and N-(2-(3,5-di-tert-butyl-4-hydroxyphenyl)-2-oxoethyl)isatin (32 μg/mL) exerted good activity against Staphylococcus aureus.

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.

Synthesis, biological activity and modeling study of some thiopyrimidine derivatives and their platinum(II) and ruthenium(III) metal complexes

2015 ◽  
Vol 70 (5) ◽  
pp. 343-353 ◽  
Author(s):  
Najim A. Al-Masoudi ◽  
Azhar Abbas ◽  
Mohammed J.B. Al-Asadi
Keyword(s):  
Escherichia Coli ◽  
Amino Acids ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Biological Activity ◽  
Metal Complexes ◽  
Hiv Reverse Transcriptase ◽  
Pyrimidine Derivatives ◽  
Hiv Replication ◽  
Hiv 1

AbstractA new series of 6-amino-5-(aryldiazenyl)-N1,N3-dimethyl-2-thioxo-pyrimidin-4-one derivatives 17–27 and the N1-methyl-azothiopyrimidine analog 28 were synthesized from the pyrimidine derivatives 4 and 5, respectively, via diazotization reaction, with various amines. The platinum(II) metal complexes [bis(4-amino-N3-methyl-6-oxo-2-thioxo-pyrimidin-1-yl)]Pt(II) (29) and [(6-amino-5-(4-R-phenyl)diazenyl)-N1,N3-dimethyl-2-thioxo-pyrimidin-4-one)]Pt(II)Cl2 derivatives 30–33 were prepared from the treatment of 5 and the azo analogs 17 and 21–23 with PtCl2, respectively. Analogously, 5 and 17 were treated with RuCl3·3H2O to give the Ru(III) complexes 34 and 35, respectively. The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. The results revealed that 26 and 30 were the only compounds in the series inhibiting HIV replication in cell cultures with an IC50 value of >2.07 and >3.02 μg mL–1, respectively. The molecular modeling interactions of 26 with some amino acids of HIV reverse transcriptase were studied. In addition, the antibacterial activity of 17–35 and 31–33 against Staphylococcus aureus and Escherichia coli was evaluated.

scholarly journals Synthesis of chalcone-based pyrimidine derivatives and their antimicrobial activity

2021 ◽  
Vol 57 (4) ◽  
pp. 431-437
Author(s):  
D. S. Martsinkevich ◽  
K. F. Chernyavskaya ◽  
V. A. Tarasevich
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Candida Tropicalis ◽  
Good Activity ◽  
Pyrimidine Derivatives ◽  
Antimicrobial Substances

A series of substituted chalcones and pyrimidine derivatives on their base was synthesized. Obtained compounds were tested for antimicrobial activity and ability to increase activity of known antimicrobial substances. Pyrimidine products shown good activity against Staphylococcus aureus and Candida tropicalis. These compounds also could increase activity of modified polyguanidines against Staphylococcus aureus.

Biological Screening of Zizyphus rugosa and Zizyphus oenoplia extractives

1970 ◽  
Vol 4 (2) ◽  
Author(s):  
M Shoeb ◽  
MIR Mamun ◽  
N Nahar ◽  
M Mosihuzzaman
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Methanol Extract ◽  
Salmonella Typhi ◽  
Moderate Activity ◽  
Good Activity ◽  
Biological Screening ◽  
Inhibitory Activities ◽  
Ethyl Acetate Extracts

Different extracts of the leaves and barks of Zizyphus rugosa and Zizyphus oenoplia were studied for their antibacterial, antifungal, and b-glucuronidase inhibitory activities. The methanol extract of Z. rugosa bark showed significant antibacterial activity against Streptococcus pyogens, Staphylococcus aureus and Pseudomonas aerogenes whereas the methanol extract of leaves demonstrated moderate activity against Salmonella typhi. The chloroform and methanol extracts of Z. oenoplia showed good activity against a few bacteria strains. The chloroform extracts of the barks and leaves of Z. rugosaalso showed antifungal activity. The methanol and ethyl acetate extracts of the bark of Z. rugosa revealed significant b-glucuronidase inhibitory activity. Lupeol, betuline, betulinaldehyde and betulinic acid, isolated from Z. rugosa, also showed good activity against a few bacteria. Key words: Zizyphus rugosa, Zizyphus oenoplia, Antibacterial, Antifungal, b-glucuronidase inhibition Dhaka Univ. J. Pharm. Sci. Vol.4(2) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

scholarly journals Antimicrobial assesment of aroylhydrazone derivatives in vitro

2019 ◽  
Vol 69 (2) ◽  
pp. 277-285 ◽  
Author(s):  
Saša Polović ◽  
Vanja Ljoljić Bilić ◽  
Ana Budimir ◽  
Darko Kontrec ◽  
Nives Galić ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Biofilm Formation ◽  
Good Activity ◽  
E Coli ◽  
Fluconazole Resistant ◽  
Gentamicin Sulphate

Abstract Aroylhydrazones 1–13 were screened for antimicrobial and antibiofilm activities in vitro. N′-(2-hydroxy-phenylmethylidene)-3-pyridinecarbohydrazide (2), N′-(5-chloro-2-hydroxyphenyl-methylidene)-3-pyridinecarbohydrazide (10), N′-(3,5-chloro-2-hydroxyphenylmethylidene)-3-pyridinecarbohydrazide (11), and N′-(2-hydroxy-5-nitrophenylmethylidene)-3-pyridinecarbohydrazide (12) showed antibacterial activity against Escherichia coli, with MIC values (in µmol mL−1) of 0.18–0.23, 0.11–0.20, 0.16–0.17 and 0.35–0.37, resp. Compounds 11 and 12, as well as N′-(2-hydroxy-3-methoxyphenylmethylidene)-3-pyridinecarbohydrazide (6) and N′-(2-hydroxy-5- methoxyphenylmethylidene)-3-pyridinecarbohydrazide (8) showed antibacterial activity against Staphylococcus aureus, with the lowest MIC values of 0.005–0.2, 0.05–0.12, 0.06–0.48 and 0.17–0.99 µmol mL−1. N′-(2-hydroxy-5-methoxyphenylmethylidene)-3-pyridinecarbohydrazide (7) showed antifungal activity against both fluconazole resistant and susceptible C. albicans strains with IC90 range of 0.18–0.1 µmol mL−1. Only compound 11 showed activity against C. albicans ATCC 10231 comparable to the activity of nystatin (the lowest MIC 4.0 ×10−2 vs. 1.7 × 10−2 µmol mL−1). Good activity regarding multi-resistant clinical strains was observed for compound 12 against MRSA strain (MIC 0.02 µmol mL−1) and compounds 2, 6 and 12 against ESBL+ E. coli MFBF 12794, with the lowest MIC for compound 12 (IC50 0.16 µmol mL−1). Anti-biofilm activity was found for compounds 2 (MBFIC 0.015–0.02 µmol mL−1 against MRSA) and 12 (MBFIC 0.013 µmol mL−1 against EBSL+ E. coli). In the case of compound 2 against MRSA biofilm formation, MBFIC values were comparable to those of gentamicin sulphate, whereas in the case of compound 12 and EBSL+ E. coli even more favourable activity compared to gentamicin was observed.

Antibacterial Activity of Desert Truffles from Saudi Arabia Against Staphylococcus aureus and Pseudomonas aeruginosa

2017 ◽  
Vol 19 (2) ◽  
pp. 121-125 ◽  
Author(s):  
Domenico Schillaci ◽  
Maria Grazia Cusimano ◽  
Stella Maria Cascioferro ◽  
Vita Di Stefano ◽  
Vincenzo Arizza ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antibacterial Activity ◽  
Saudi Arabia ◽  
Desert Truffles

Antibacterial Activity of Thujaoccidentalis,ThujaorientalisandChamaecyparisobtusa

2017 ◽  
Vol 8 (03) ◽  
Author(s):  
Kyoung- Sun Seo ◽  
Seong Woo Jin ◽  
Seongkyu Choi ◽  
Kyeong Won Yun
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Antibacterial Agent ◽  
Methanol Extract ◽  
The Other ◽  
Diffusion Method ◽  
E Coli ◽  
Agar Diffusion ◽  
Agar Diffusion Method ◽  
Crude Methanol Extract

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.

Chemical Composition and Antibacterial Activity of Essential Oils of Three Medicinal Plants from Algerian Semi-Arid Climatic Zone

2018 ◽  
Vol 16 (S1) ◽  
pp. S155-S163 ◽  
Author(s):  
S. Mehalaine ◽  
O. Belfadel ◽  
T. Menasria ◽  
A. Messaili
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antibacterial Activity ◽  
Chemical Composition ◽  
Essential Oil ◽  
Essential Oils ◽  
Rosmarinus Officinalis ◽  
Salvia Officinalis ◽  
Thymus Algeriensis

The present study was carried out to determine, for the first time, the chemical composition and antibacterial activity of essential oils derived from the aerial parts of three aromatic plants Thymus algeriensis Boiss & Reut, Rosmarinus officinalis L., and Salvia officinalis L. growing under semiarid conditions. The essential oils were chemically analyzed and identified by gas chromatography (GC) and GC/ mass spectrometry (GC/MS) and their antimicrobial activity was individually evaluated against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa using both agar disk diffusion and agar dilution methods. The major constituents of Thymus algeriensis essential oil were identified as camphor (13.62%), 1,8-cineol (6.00%), borneol (5.74%), viridiflorol (4.00%), and linalool (3.93%). For Rosmarinus officinalis essential oil, 48 compounds were characterized, of which the main constituents were camphor (17.09%), Z-β-ocimene (10.88%), isoborneol (9.68%), α-bisabolol (7.89%), and borneol (5.11%). While, Salvia officinalis essential oil was characterized by β-thujone (16.44%), followed by viridiflorol (10.93%), camphor (8.99%), 1,8-cineol (8.11%), trans-caryophyllene (5.85%), and α-humulene (4.69%) as the major components. Notably, results from antibacterial screening indicated that Thymus algeriensis and Salvia officinalis essential oils exhibited a strong inhibitory effect against both Escherichia coli and Staphylococcus aureus compared to Rosmarinus officinalis essential oil. Further, less activity was recorded against Pseudomonas aeruginosa for the three tested essential oils.

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