Synthesis of s-Triazine-Based Thiazolidinones as Antimicrobial Agents

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)

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.


2003 ◽  
Vol 58 (11-12) ◽  
pp. 850-854 ◽  
Author(s):  
Ayşen Özdemir Türk ◽  
Meral Yılmaz ◽  
Merih Kıvanç ◽  
Hayrettin Türk

Abstract In this study, the antimicrobial activity of the acetone, diethyl ether and ethanol extracts of the lichen Cetraria aculeata has been investigated. The extracts were tested against twelve bacteria and eight fungi and found active against Escherichia coli, Staphylococcus aureus, Aeromonas hydrophila, Proteus vulgaris, Streptococcus faecalis, Bacillus cereus, Bacillus subtilis, Pseudomonas aeruginosa, Listeria monocytogenes. No antimicrobial activity against the fungi was detected. It was determined that only one substance in the extracts has antimicrobial activity and it was characterized as protolichesterinic acid. The MICs of the extracts and protolichesterinic acid were also determined.


2020 ◽  
pp. 79-85
Author(s):  
Aleksandr Alekseyevich Efremov ◽  
Irina Dement'yevna Zykova ◽  
Natal'ya Sergeyevna Korosteleva

By the method of exhaustive hydroponically obtained essential oil from beans of Heracleum dissectum Ledeb., growing in the Krasnoyarsk region. Separate fractions of oil were obtained: the first after 45 minutes from the beginning of distillation, the second – after 2 hours, the third-after 5 hours, the fourth fraction was collected after the end of hydro-distillation. The component composition of both whole essential oil and its separate fractions was studied. The main components are octyl acetate (60.0%), octyl-2-methylpropanoate (10.2%), n-hexyl-2-methylbutanoate (9.0%). The main amount of octyl acetate (64.7%) is concentrated in the first fraction of the oil. The antimicrobial activity of various fractions of essential oil of borscht dissected against strains of opportunistic microorganisms: Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Staphylococcus aureus 209p, MRSA, Proteus vulgaris. It was found that, depending on the duration of isolation, the antimicrobial activity of essential oil fractions in relation to Staphylococcus aureus 209p, MRSA and Pseudomonas aeruginosa decreases, and in relation to Escherichia coli, Klebsiella pneumoniae and Proteus vulgaris increases. The most pronounced inhibitory effect of the third and fourth fractions of essential oil against Klebsiella pneumonia. The antiradical activity of all studied samples of borscht essential oil dissected in reaction with stable free 2,2-diphenyl-1-picrylhydrazyl radical was established. The first fraction showed minimal antiradical activity (15.1%), the fourth – maximum (49.2%).


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.


2017 ◽  
Vol 8 (1) ◽  
Author(s):  
Renu Narendra Jaisinghani

Quercetin is a polyphenolic flavonoid with potential chemoprotective properties. In the present work its antibacterial properties were studied against Staphylococcus aureus, Escherichia coli, Shigella flexneri, Proteus vulgaris, Pseudomonas aeruginosa, Lactobacillus casei var shirota by broth dilution method. Quercetin inhibited S. aureus, P. aeruginosa at concentration 20 mcg/mL while P. vulgaris and E. coli were inhibited at concentration 300 mcg/mL and 400 mcg/mL respectively. Shigella flexneri and Lactobacillus casei var shirota were completely indifferent even at concentration of 500 mcg/mL.


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.


2010 ◽  
Vol 59 (1) ◽  
pp. 49-53 ◽  
Author(s):  
BOGUMIŁ BRYCKI ◽  
ZOFIA DEGA-SZAFRAN ◽  
ILONA MIRSKA

The synthesis and antimicrobial activity of 31 morpholinium chlorides, divided into five series depending on the substituents attached to the nitrogen atom, N-carboxyalkyl-morpholinium chlorides (1a-e), N-carbalkoxymethyl-N-methyl-morpholinium chlorides (2a-f), N-carbethoxymethyl-N-alkyl-morpholinium chlorides (3a-g), N-carbalkoxymethyl-N-dodecyl-morpholinium chlorides (4a-f) and N-carboxymethyl-N-alkyl-morpholinium chlorides (5a-g) is reported. The compounds investigated were tested for antimicrobial activity against Staphylococcus aureus, Escherichia coli, Proteus vulgaris, Pseudomonas aeruginosa, Candida albicans and Trichophyton menthagrophytes. The most active are compounds with a long N-alkyl group and with the substituent CH2COOC(n)H(2n-1) (n = 8-16).


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.


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