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

Author(s):  
D. S. Martsinkevich ◽  
K. F. Chernyavskaya ◽  
V. A. Tarasevich

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.

Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2370 ◽  
Author(s):  
Vladimir N. Koshelev ◽  
Olga V. Primerova ◽  
Stepan V. Vorobyev ◽  
Ludmila V. Ivanova

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.


Author(s):  
Cristina Al-Matarneh ◽  
Irina Rosca ◽  
Sergiu Shova ◽  
Ramona Danac

New fused pyrrolo-phenanthroline type derivatives were synthesized, in two steps, from 1,10-phenanthroline and evaluated for antimicrobial activity and fluorescence properties. Our synthetic approach involved a 3+2 dipolar-cycloaddition of some selected N-substituted 1,10-phenanthrolin-1-ium ylides, (m)ethoxycarbonyl and cyano (1,2-di)substituted acetylenes and alkenes, respectively. The structures of compounds were supported by analytical and spectroscopic data. Molecular structures of four compounds have also been also determined by monocrystal XRD analyses. All synthesized compounds were then evaluated for their potential antimicrobial activity against Staphylococcus aureus ATCC25923, Escherichia coli ATCC25922 and Candida albicans ATCC10231. Two of the compounds demonstrated good activity against the above tested strains.


2012 ◽  
Vol 30 (No. 4) ◽  
pp. 330-335 ◽  
Author(s):  
K. Trivedi ◽  
R. Sedmíková ◽  
R. Karpíšková

In total 228 enterococci strains isolated from food were studied. Enterococcus faecalis, E. faecium, and E. casseliflavus were found to be the dominant strains while E. durans and E. mundtii were present in a smaller extent. Antimicrobial activity determined by double layer technique revealed that 150 (65.7%) strains showed antimicrobial activity against the individual tested pathogenic strains of Listeria monocytogenes, Staphylococcus aureus, and methicilin resistant S. aureus (MRSA). Cell-free neutralised supernatants (CFNS) were prepared from 150 potential bacteriocin producers. Of these 150, CFNS 107 (71.3%) strains were active in the bacteriocin production against one or more pathogenic strains tested. S. aureus and MRSA were found to be more sensitive to the antimicrobial substances than L. monocytogenes. Multiplex PCR for the detection of seven virulence genes in bacteriocin producing strains showed that 47.6% of strains were able to amplify one or more virulence genes. E. faecalis was the most virulent species. The presence of tyrdc gene was seen in all bacteriocin producing strains. None of the strains carried genes encoding the resistance to vancomycin.  


2010 ◽  
Vol 5 (5) ◽  
pp. 1934578X1000500 ◽  
Author(s):  
Osman Üçüncü ◽  
Nuran Kahriman ◽  
Salih Terzioğrlu ◽  
Şengül Alpay Karaoğrlu ◽  
Nurettin Yaylı

The chemical composition of the essential oils of Senecio othonnae, S. racemosus, and S. nemorensis obtained by hydrodistillation of fresh flowers were analysed by GC-FID and GC-MS. A total of seventy-six compounds were identified, constituting over 83.1%, 97.7% and 86.8% of the total oil composition of the flowers of S. othonnae, S. racemosus, and S. nemorensis. The main components of the oils were caryophyllene oxide (18.6%), ( E)-β-farnesene (21.6%), and γ-curcumene (42.8%), respectively. Sesquiterpene hydrocarbons were the main group of constituents of all three species, forming 34.6%, 73.2%, and 81.8% of the oils, respectively. The oils of S. othonnae, and S. nemorensis showed antimicrobial activity against Bacillus cereus, Staphylococcus aureus, Enterococcus faecalis, and Candida tropicalis, but that of S. racemosus was only active against Candida tropicalis.


2017 ◽  
Vol 82 (4) ◽  
pp. 367-377 ◽  
Author(s):  
Demet Coskun ◽  
Seher Gur ◽  
Mehmet Coskun

The aim of this study was the preparation of 1,1?-(2,5-thiophenediyl) bis[1-(2-benzofuranyl)methanone] (2), the corresponding diketoxime (3), and the ether and ester derivatives (4a?e) of the diketoxime. These compounds were prepared in good yields. Minimum inhibitory concentrations (MIC) of the synthesized compounds 1?4 were determined against Salmonella enterica subsp. enterica serovar Typhimurium, Escherichia coli and Staphylococcus aureus. Among the synthesized compounds, 1 and 4e showed good activity against E. coli, S. enterica and S. aureus.


2021 ◽  
Author(s):  
FANTE BAMBA ◽  
Tchambaga Camara ◽  
Coulibali Sioménan ◽  
Sagne Jacques Akpa ◽  
Adjou Ané

Abstract SecA, a key component of bacterial Sec-dependent secretion pathway, is an attractive target for exploring novel antimicrobials. Along this line, we reported optimization of a hit bistriazole (SCA 21) which has been previously identified as a SecA inhibitor. Herein we describe the synthesis of some novel triazole-pyrimidine derivative by structural modification of SCA 21. Some of them have been evaluated for their antimicrobial activity against against Escherichia coli NR698 (a leaky mutant), Staphylococcus aureus and Bacillus anthracis Sterne.


2021 ◽  
Vol 4 (1) ◽  
pp. 32-38
Author(s):  
Lia Yulia Budiarti ◽  
Isnaini Isnaini ◽  
Puteri Dayana ◽  
Norma Sari ◽  
Nur Almira R. S.

Stenochlaena palustris and Sauropus androgynus are known to contains antimicrobial substances such as flavonoids, saponins and tannins compounds.The purpose of this study was to analyzes the antimicrobial activity of young and old leaf infusions of S. palustris and S. androgynus leaves against Staphylococcus aureus, Escherichia coli and Candida albicans. Analyze the antibacterial activity of a single preparations with a combination preparation of S.palustris (SP) and S.androgynus (SA) leaves infusion against S.aureus, E.coli and C.albicans. Leaves of S.palustris young part (SP1) taken 0-10 cm from shoots and old parts (SP2) 11-20 cm from shoots, while leaves of S.androgynus young part (SA1) leaves number 1 - 10 from the top and the old part (SA2) leaves number 11-20 from the top. The results showed that a single infusion of SP1 75% and SP2 75%, SA1 90% and SA2 90%, and a combination of SP1 75% and SA1 75%, SP2 75% and SA2 75% have the same activity as ampicillin in S.aureus. Single infusion of SP1 90% and SP2 90%, SA1 90% and SA2 90%, combination of SP1 75% and SA1 80% and the combination of SP2 80% and SA2 60% have the same activity as ciprofloxacin in E. coli. Single infusion of SP1 90% and SP2 90%, and a combination of SP1 80% and SA1 80%, SP2 80% and SA2 80% have the same activity as ketoconazole in C.albicans. The difference in activity due to differences in leaf parts used only occurred in E. coli, whereas in S.aureus and C.albicans (p <0.05).


2020 ◽  
Vol 32 (9) ◽  
pp. 2298-2302
Author(s):  
SHOBHANA A. GADARA ◽  
KARTIK D. LADVA

A new series of triazolo[4,3-a]pyimidine derivatives via solid phase multicomponent reaction between 3-oxo-N-(4-(3-oxomorpholino)- phenyl)butanamide, aromatic aldehyde and aminoazole is reported. All the synthesized compounds have been characterized by elemental analysis and spectral analyses. Moreover, the synthesized compounds were also screened for their antibacterial activity against Staphylococcus aureus MTCC-96, Escherichia coli MTCC-443, Bacillus subtilis MTCC-441, Pseudomonas aeruginosa MTCC 1688, and antifungal activity against Aspergillus niger MTCC-282 and Penicillium sp. at different concentration and compared with standards drugs. The minimum inhibition concentration (MIC) of the compounds was studied by micro-broth dilution method.


Coatings ◽  
2019 ◽  
Vol 9 (8) ◽  
pp. 494 ◽  
Author(s):  
Klein ◽  
Alzagameem ◽  
Rumpf ◽  
Korte ◽  
Kreyenschmidt ◽  
...  

Due to global ecological and economic challenges that have been correlated to the transition from fossil-based to renewable resources, fundamental studies are being performed worldwide to replace fossil fuel raw materials in plastic production. One aspect of current research is the development of lignin-derived polyols to substitute expensive fossil-based polyol components for polyurethane and polyester production. This article describes the synthesis of bioactive lignin-based polyurethane coatings using unmodified and demethylated Kraft lignins. Demethylation was performed to enhance the reaction selectivity toward polyurethane formation. The antimicrobial activity was tested according to a slightly modified standard test (JIS Z 2801:2010). Besides effects caused by the lignins themselves, triphenylmethane derivatives (brilliant green and crystal violet) were used as additional antimicrobial substances. Results showed increased antimicrobial capacity against Staphylococcus aureus. Furthermore, the coating color could be varied from dark brown to green and blue, respectively.


2021 ◽  
Vol 43 ◽  
pp. e49786
Author(s):  
Claudio Baltazar de Sousa ◽  
Erika Alves Fonseca Amorim ◽  
Rita de Cassia Mendonça Miranda

. Endophytic fungi colonize the interior of plants without causing damage and act in symbiosis with their host. They are also potential sources of compounds with potential applications in industry, agriculture, and medicine, Thus, this study aimed to isolate and identify the endophytic fungi medicinal plant Talinum triangulare and evaluate its potential for the production of antimicrobial substances using the disk diffusion technique and testing in liquid medium front of Staphylococcus aureus ATCC SA 6538, Pseudomonas aeruginosa ATCC PA 0030, and Corynebacterium diphtheria ATCC 27012. Corynebacterium diphtheria was isolated from 3 fungi of the genus Trichoderma and Penicillium, with only the genus Trichoderma fungi showing antimicrobial activity.


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