scholarly journals Synthesis and Evaluation of Some New Thiazolidin-4-One Derivatives as Potential Antimicrobial Agents

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.

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.


Author(s):  
Powar Priyatama V ◽  
Powar Trupti A

The growing phenomenon of antibiotic resistance, particularly to pathogenic microorganisms, in current medicine, has directed the concern of scientists for finding novel antimicrobial agents from plant origin with negligible side effect. The present study was aimed to phytochemical investigation and antimicrobial activity of seed extract of Datura stramonium in sequentially with different organic solvents. For this, antimicrobial properties were tested against bacteria Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumonia and Bacillus subtilis by cup plate method. Among the tested bacterial Klebsiella pneumoniae was the most inhibited majorly with the chloroform extract. Datura stramonium chloroform seed extract produced maximum zone of inhibition 26 mm against Klebsiella pneumoniae and 12 mm against Bacillus subtilis and 13 mm against Escherichia coli. Datura Stramonium methanol seed extract produced maximum zone of inhibition 27 mm against Pseudomonas aeruginosa and 15 mm against Bacillus subtilis, 14 mm against Staphylococcus aureus and 19 mm against Escherichia coli. Datura stramonium petroleum ether seed extract produced 16 mm zone of inhibition against Escherichia coli. Datura stramonium aqueous seed extract exhibits 24 mm zone of inhibition against Bacillus subtilis. All the experienced solvent extracts showed potential antimicrobial activity Index against various tested microorganisms. Owning to the results, it can be concluded that the extracts of the Datura stramonium can be used to design different herbal antimicrobial agents.


2020 ◽  
Vol 38 ◽  
Author(s):  
K. WAHEED ◽  
S.K. MUHAMMAD ◽  
A. SHOMAILA ◽  
Z. MUHAMMAD ◽  
U. IZHAR ◽  
...  

ABSTRACT: Medicinal Plants have been used throughout the world by human beings as a drug and remedies for various diseases since time immemorial. A study was planned to count into the antimicrobial activity and phytochemical screening of Euphorbia helioscopia. The plants were gathered and tested against some standard strains and some human pathogenic microorganisms i.e Escherichia coli, Bacillus Subtilis, Staphylococcus aureus, Klebsiella pneumoniae, Salmonella typhi, Pseudomonas aeruginosa and three fungal strain Trichoderma, R hizopus nigricans, Aspergillus niger. The concentrations of extracting samples (500 and 1,000 mg mL-1) were used against pathogens. Ciprofloxacin was used as positive control in case of bacterial strains and Colfrimazol was used against the fungal strain while dimethyl sulfoxide as negative control. The outcomes indicated that the positive wells potency of Water extract had a 36 mm diameter of zone of inhibition against Escherichia coli and ethanol extract at 1,000 mg mL-1 had maximum (34 mm) zone of inhibition against Bacillus subtilus (36 mm) zone of inhibition against Klebsiella pneumonia and 33 mm of zone of inhibition against Trichoderma harzianum. Likewise, water extract at a concentration of 1,000 mg mL-1 resulted highest value of zone of inhibition (36 mm) against Staphylococcus aureus, a zone of inhibition ( mm) against Salmonella typhi, 36 mm zone of inhibition against Pseudomonas aeruginosa, (32 mm) zone of inhibition against Rhizopus nigricans, a 34 mm zone of inhibition against Acremonium and (34 mm) zone of inhibition against Aspergillus niger. The most susceptible bacteria were K. pneumonia and Bacillus subtilis, while E. coli was the most resistant bacteria and showed zone of inhibition. The ethanolic extract had tannins, lipid, total proteins, carbohydrates, flavonoids, Alkaloid and polyphenolics.


2012 ◽  
Vol 67 (3-4) ◽  
pp. 108-122
Author(s):  
Divyesh Patel ◽  
Rahul Patel ◽  
Premlata Kumari ◽  
Navin B. Patel

5A novel series of thiazolidinone derivatives, namely 4-{4-dimethylamino-6-[4-oxo- 2-phenyl-5-(4-pyridin-2-yl-piperazin-1-ylmethyl)-thiazolidin-3-yl]-[1,3,5]-triazin-2-yloxy}- 1-methyl-1H-quinolin-2-ones, have been synthesized from the key intermediate 4-(4-amino- 6-dimethylamino-[1,3,5]-triazin-2-yloxy)-1-methyl-1H-quinolin-2-one (). Compound 5 was condensed with various aldehydes to give Schiff base derivatives, which after cyclization gave thiazolidinones that were linked with 1-pyridin-2-yl-piperazine to obtain the target compounds. The newly synthesized compounds were evaluated for their antimicrobial activity against eight bacteria (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi, Proteus vulgaris, Shigella flexneri) and four fungi (Aspergillus niger, Candida albicans, Aspergillus fumigatus, Aspergillus clavatus)


2011 ◽  
Vol 396-398 ◽  
pp. 1875-1878 ◽  
Author(s):  
Yu Ting Liu ◽  
Hai Long Guo ◽  
Da Wei Yin

Three bis-acetylferrocene schiff bases have been synthesized and characterized by IR, 1H NMR, and elemental analysis, the results conformed well with expected structures. The synthesized compounds were screened in vitro for their antimicrobial activity against three Gram-negative (Escherichia coli, Pseudomonas aeruginosa, and Salmonella typhi) and two Gram-positive (Bacillus subtilis and Staphylococcus aureus) bacterial strains. The results showed that these compounds are show excellent antimicrobia activities against Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi ,Bacillus subtilis,Staphylococcus aureus.


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.


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.


2018 ◽  
Vol 7 (4) ◽  
pp. 392-398
Author(s):  
B.T Yunana ◽  
◽  
B. B Bukar ◽  
J. C Aguiyi ◽  
◽  
...  

The ethanol extracts of root, bark and leaf of Bridelia ferruginea was investigated for antibacterial activity against clinical isolate of Staphylococcus aureus and Escherichia coli. The extracts had significant antibacterial activity in vitro at concentration of 25 mg/ml, 50 mg/ml, 100 mg/ml and 200 mg/ml and in vivo at dose of 50 mg/kg and 100 mg/kg. The root extract in vitro had the highest zone of inhibition, followed by the bark extract for both Staphylococcus aureus and Escherichia coli. The concentration of 200 mg/ml had the highest zone of inhibition in vitro. The minimum inhibitory concentration (MIC) showed a decreasing inhibitory effect of the plant extracts for both Staphylococcus aureus and Escherichia coli as the concentration decreases with root having 3.125 mg/ml, bark having 6.25 mg/ml and leaf having 25 mg/ml for Staphylococcus aureus and Escherichia coli. Likewise, the minimum bactericidal concentration (MBC) showed decreasing bactericide effects with decrease concentration with root having 12.5 mg/ml, bark having 12.5 mg/ml and leaf having 25 mg/ml for Escherichia coli while root had 6.25mg/ml, bark had 12.5mg/ml and leaf had 25mg/ml for Staphylococcus aureus. The in vivo investigation showed that the root and bark extract exhibited antibacterial activity on both Staphylococcus aureus and Escherichia coli at doses of 100mg/kg and 50mg/kg; the root extract had higher activity than the bark and root/bark combined. The dose of 100 mg/kg had the highest colonies reduction for Staphylococcus aureus and Escherichia coli in vivo. Preliminary phytochemical screening of root, bark and leaves of Bridelia ferruginea revealed the presence of tannins, flavonoids, carbohydrates, cardiac glycoside (root, bark and leaves), saponins (root and bark). The presence of tannins, saponins, flavonoid, cardiac glycoside and carbohydrate in the bark and root extracts of the plant indicates that the bark and root extracts were pharmacological importance


2011 ◽  
Vol 76 (12) ◽  
pp. 1597-1606 ◽  
Author(s):  
Nemanja Trisovic ◽  
Bojan Bozic ◽  
Ana Obradovic ◽  
Olgica Stefanovic ◽  
Snezana Markovic ◽  
...  

A series of twelve 3-substituted-5,5-diphenylhydantoins was synthesized, including some whose anticonvulsant activities have already been reported in the literature. Their antiproliferative activities against HCT-116 human colon carcinoma cells were evaluated to determine structure-activity relationships. Almost all of the compounds exhibited statistically significant antiproliferative effects at a concentration of 100 ?M, while the derivative bearing a benzyl group was active even at lower concentrations. Moreover, their in vitro antibacterial activities against Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923 and clinical isolates of Escherichia coli, Proteus mirabilis, Pseudomonas aeruginosa, Enterococcus faecalis and Staphylococcus aureus were evaluated. Only the 3-iso-propyl and 3-benzyl derivatives showed weak antibacterial activities against the Gram-positive bacterium E. faecalis and the Gram-negative bacteria E. coli ATCC 25922 and E. coli.


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)


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