scholarly journals Synthesis and Antibacterial Activity of New Azole, Diazole and Triazole Derivatives Based on p-Aminobenzoic Acid

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2597
Author(s):  
Birutė Sapijanskaitė-Banevič ◽  
Vykintas Palskys ◽  
Rita Vaickelionienė ◽  
Jūratė Šiugždaitė ◽  
Povilas Kavaliauskas ◽  
...  

The p-aminobenzoic acid was applied for the synthesis of substituted 1-phenyl-5-oxopyrrolidine derivatives containing benzimidazole, azole, oxadiazole, triazole, dihydrazone, and dithiosemicarbazide moieties in the structure. All the obtained compounds were evaluated for their in vitro antimicrobial activity against Staphylococcus aureus, Bacillus cereus, Listeria monocytogenes, Salmonella enteritidis, Escherichia coli, and Pseudomonas aeruginosa by using MIC and MBC assays. This study showed a good bactericidal activity of γ-amino acid and benzimidazoles derivatives. The antimicrobial activity of the most promising compounds was higher than ampicillin. Furthermore, two benzimidazoles demonstrated good antimicrobial activity against L. monocytogenes (MIC 15.62 µg/mL) that was four times more potent than ampicillin (MIC 65 µg/mL). Further studies are needed to better understand the mechanism of the antimicrobial activity as well as to generate antimicrobial compounds based on the 1-phenyl-5-oxopyrrolidine scaffold.

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
B. A. Baviskar ◽  
S. S. Khadabadi ◽  
S. L. Deore

A new series ofN-{4-methyl-5-[4-(4-oxo-2-phenyl(1,3-thiazolidin-3-yl)]-5-sulfanyl(1,2,4-triazol-3-yl)-1,3-thiazol-2-yl }acetamide (7a-l) was synthesized in order to determine their antimicrobial activity and feasible structure–activity relationships. The compounds were synthesized in good yield and the structures of all newly synthesized compounds were established on the basis of their IR,1HNMR, and elemental analysis. The synthesized compounds were testedin vitroantibacterial activity againstStaphylococcus aureus,Escherichia coli,Pseudomonas aeruginosaandSalmonella typhiand antifungal activity againstAspergillus niger,Candida albicansby measuring the zone of inhibition in mm.


2020 ◽  
Vol 22 (1) ◽  
pp. 43 ◽  
Author(s):  
Т.V. Kharlamova ◽  
R.B. Seidakhmetova ◽  
K.D. Praliyev

The present study is a continuation of the scientific research works for the synthesis of anthraquinonе-containing derivatives with cyclic ring systems by the interaction of 1,2,4-trihydroxyanthraquinone (purpurin) with cyclic carboxylic acid chlorides. Series of purpurin esters containing a saturated cyclic fragment was studied for antibacterial activity about museum strains of microorganisms. The effects of these preparations in vitro about Staphylococcus aureus ATCC 6538, Bacillus subtilis ATCC 6633, Escherichia coli ATCC 25922, Pseudomonas aeruginosa АТСС 27853 and fungus Сandida albicans АТСС 10231 were studied. It has been found that the compounds with the cyclohexane fragment have possess an antimicrobial activity with strains of microorganisms Staphylococcus aureus АТСС 6538 for which the MIC value was 31.25 μg/ml.


2015 ◽  
Vol 10 (6) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Corina Danciu ◽  
Florin Borcan ◽  
Codruta Soica ◽  
Istvan Zupko ◽  
Erzsébet Csányi ◽  
...  

In recent years polyurethane microstructures (PM) have gained increasing attention in the pharmaceutical field due to the importance of their practical application. Since finding that such a formulation with genistein could improve its applications, we have conducted a preliminary study regarding the in vitro antiproliferative (MCF7, MDA-MB-231 and T47D) and antimicrobial ( Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis (D), Bacillus subtilis, B. cereus, and Candida albicans) activity in order to test whether polyurethane micro structuresre present a good option for further modulation of genistein's bioavailability. It was concluded that the polyurethane micro structures are a bad in vitro partner for the isoflavone genistein.


2019 ◽  
Vol 18 (2) ◽  
pp. 223-232
Author(s):  
AO Shittu ◽  
A Aliyu ◽  
MS David ◽  
NS Njinga ◽  
HI Ishaq

In order to authenticate and ascertain the various claim by the rural dwellers that depend on chewing sticks for their oral hygiene and protection against innumerable diseases, the antibacterial activity of the roots of Fagara zanthoxyloides and Distemonanthus benthamianus were evaluated. Preliminary phytochemical screening was carried out using standard methods. In-vitro antibacterial activity of the methanol extracts of both plants was also carried out using the agar well diffusion method against standard strains of Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Escherichia coli ATCC 25922, Salmonella typhii ATCC 14028, Citrobacter freundii ATCC 8090 and also some clinical isolates of Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis at different concentrations and ratios. Preliminary phytochemical screening showed that the extracts contained alkaloids, saponin, tannins, steroids, flavonoids, anthraquinones, cardiac glycosides and phenol. All the test microorganisms were susceptible to the inhibitory effect of the extracts at concentrations of 200 mg/ml and 500 mg/ml. F. zanthoxyloides had better antimicrobial activity with zones of inhibition ranging from 21.0 to 26.0 mm at 200 mg/ml and 24.3 to 29.3 mm at 500 mg/ml while D. benthamianus had zones of inhibition ranging from 17.7 to 26.7 mm at 200 mg/mL and 19.0 to 26.7 mm at 500 mg/mL. Some of the test microorganisms were resistant to the standard antibiotics (cefuroxime, ciprofloxacin, ofloxacin and gentamicin). Combinations of the extracts in ratios 50:50 and 75:25 yielded no increase in activity. The MIC and MBC for D. benthamianus ranged from 6.25 mg/ml to 100 mg/mL and 25 to 200 mg/ml, respectively while that of F. zanthoxyloides ranged from 1.56 mg/ml to 12.5 mg/mL and 50 to 200 mg/ml, respectively. The antimicrobial activity demonstrated by F. zanthoxyloides and D. benthamianus indicates that they would be valuable in the management of urinary, respiratory and gastrointestinal tracts infections while at the same time helping to mitigate the problem of antimicrobial resistance. Phenolic compounds of plants, among them flavonoids are the chief constituents, which have potent antioxidant activities Dhaka Univ. J. Pharm. Sci. 18(2): 223-232, 2019 (December)


Author(s):  
Rajanikanth Garapati ◽  
N. Ramesh

Objective: In vitro investigated the potential of methanol extracts of micro-propagated C. orchiodes in the antimicrobial property against the three gram-negative bacteria, two gram-positive and one fungal filament.Methods: The micro propagated callus methanol extract was examined against Escherichia coli, Proteus vulgaris, Salmonella typhimurium, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus cereus and Candida albicans. The zone of inhibitions are determined at 10 mg/ml concentration of methanol extracts of callus on agar well plate and MIC against tested microorganism.Results: The highest antibacterial activity recorded in Staphylococcus aureus Bacillus cereus and followed by Candida albicans. Antibacterial activity of leaf extracts of A. reticulata was also significant against the tested microorganisms Escherichia coli, Salmonella typhi, Proteus vulgaris, Pseudomonas aeruginosa compared to ciprofloxacin.Conclusion: Based on the above observations, these extracts were further evaluated for their effect on microorganisms causing infections like typhoid fever, urinary tract infections, septicemia, toxic shock syndrome, skin infection, nosocomial infection, arthritis and diarrhoea. The results also suggest that these plants serve a therapeutic purpose in the treatment bacterial infections.


10.3823/819 ◽  
2018 ◽  
Vol 8 (1) ◽  
Author(s):  
Fatima El Malki ◽  
Kamal Eddaraji ◽  
Rajae Alloudane ◽  
Hassane Greche ◽  
Haiat Essalmani ◽  
...  

Introduction: Medicinal plants are plentiful of bioactive molecules effective against multi-resistance bacteria. The aims of this study were to assess the in vitro antimicrobial activities of essential oils extracted from three Moroccan aromatic plants. Methodology: Analysis of essential oils of Origanum compactum, Rosmarinus officinalis and Pelargonium asperum, collected from different localities in Morocco, were performed using a GC-MS spectrophotometry. Antibacterial activity was evaluated in vitro for five clinical multi-resistant isolates. Results: Origanum showed strong antibacterial activity against tested strains except Pseudomonas aeruginosa while Rosmarinum showed a bactericidal effect against Acinetobacter baumanii, Escherichia coli and Staphylococcus aureus. Pelargonium presented only slight growth inhibition of Staphylococcus aureus on solid medium, but provided bactericidal effect against Acinetobacter baumanii and Staphylococcus aureus. Interestingly, fractions F7 and F8 of Pelargonium which represented only 0.3% and 0.1% of the total mass were found bactericidal respectively against Klebsiella pneumoniae and Pseudomonas aeruginosa. Conclusions: Ours results showed that the antimicrobial activities were variables depending on the chemical composition of essential oils, the fraction used and the microorganism tested.Essential oils fractionation allows detection of bioactive substances, especially those owning antimicrobial activity, present in small quantities.


2022 ◽  
Vol 11 (1) ◽  
pp. 75-82 ◽  
Author(s):  
Iryna Myrko ◽  
Taras Chaban ◽  
Vasyl Matiychuk

A series of some new pyrazole-substituted 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines was synthesized in this study. The structures of target substances were confirmed by using 1H and 13С NMR spectroscopy, mass spectrometry and elemental analysis. The synthesized compounds have been evaluated for antimicrobial activity against five bacterial strains (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus) and two fungal strains (Candida albicans and Cryptococcus neoformans). The antimicrobial screening studies of synthesized substances established that 2 of 12 compounds show pronounced antibacterial activity against the strain Staphylococcus aureus.


2021 ◽  
Vol 2 (1) ◽  
Author(s):  
Abdulhamid Imam Tanko ◽  
Abdulgafar Olayiwola Jimoh ◽  
Muhammad Tukur Umar ◽  
Shuaibu Abdullahi Hudu

Background: Despite the availability of more researched and formulated orthodox medicines, traditional medicines remain the main source of therapy for the majority of people worldwide with some patrons concurrently using both forms unaware of the unwanted effects that may occur. Camel milk is often used alone or in combination with other orthodox medications to treat diseases. The study aimed to investigate the influence of camel milk on the antibacterial activity of ciprofloxacin. Materials and methods: The in vitro antibacterial activity of camel milk escalating doses (30μL, 100μL and 300μL) alone and in combination with Ciprofloxacin escalating doses (2mcg, 5mcg, 15mcg) against some clinical bacterial isolates (Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, Serratia marcescens) was determined using the Agar-well diffusion method. Result: Camel milk escalating doses alone showed dose-dependent antibacterial effect against all the test bacteria. However, combinations of the camel milk escalating doses and ciprofloxacin escalating doses respectively produced an antagonistic effect against all the test organisms. Conclusion: Fresh camel milk possesses antibacterial activity against Pseudomonas aeruginosa, Escherichia coli, Serratia marcescens and Staphylococcus aureus but is not recommended for combination with ciprofloxacin to treat infections caused by the above organisms.


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