scholarly journals Synthesis and biological evaluation of some new 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines as antimicrobial agents

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.

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.


2021 ◽  
Vol 5 (1) ◽  
pp. 1-9
Author(s):  
Antonio Carlos Pereira de Menezes Filho ◽  
Matheus Vinícius Abadia Ventura ◽  
Carlos Frederico de Souza Castro

Tibouchina granulosa is a species that blooms annually in several regions of Brazil. This species is still little explored in terms of phytocompounds in all organs of this plant, especially the floral organ. Flowers of T. granulosa were collected in the municipality of Rio Verde, Goiás, Brazil, in 2021. The hydroethanolic floral extract was prepared by maceration and qualitative phytochemical (colorimetric reactions and salt formation) and antibacterial analyzes performed and the results expressed in millimeters of inhibition at different concentrations in mg mL-1. Several phytochemical classes were observed with positive results, especially for alkaloids, phenolics, oxylates, saponins, carbohydrates and tannins. As for the bacterial assay, potential antibacterial activity was observed for all bacterial strains tested, except for Salmonella serovar Thyphymurium and serovar Enteritidis. Expressive inhibitions were observed for Enterococcus faecalis > Pseudomonas aeruginosa > Staphylococcus aureus and Escherichia coli at the highest concentrations between 100-50 mg mL-1. The floral extract of Tibouchina granulosa showed phytotherapeutic potential with the presence of several phytochemical groups and expressive antibacterial activity.


2018 ◽  
Vol 13 (4) ◽  
pp. 1934578X1801300
Author(s):  
Daniyar Sadyrbekov ◽  
Timur Saliev ◽  
Yuri Gatilov ◽  
Ivan Kulakov ◽  
Roza Seidakhmetova ◽  
...  

A cyclopropane derivative of limonene, (1 S, 4 S, 6 R)-7,7-dichloro-4-[(1 S)-2,2-dichloro-1-methylcyclopropyl]-1-methylbicyclo [4.1.0] heptane (compound 2), was synthesized and its structure was determined by NMR and X-ray crystallographic methods. In addition, an antimicrobial activity of the compound against Gram-positive ( Staphylococcus aureus, Bacillus subtilis) and Gram-negative ( Escherichia coli, Pseudomonas aeruginosa) bacterial strains was also scrutinized.


2021 ◽  
Vol 37 (2) ◽  
pp. 508-512
Author(s):  
Jaganmohana Rao Saketi ◽  
S N Murthy Boddapati ◽  
Raghuram M ◽  
Geetha Bhavani Koduru ◽  
Haribabu Bollikolla

The in vitroantimicrobial properties of a series of N-methyl-3-aryl indazoles (5a-5j) were screened. In this present work, we describe our efforts towards the development of potent antimicrobial activity of synthesized indazole derivatives. The antimicrobial activities of the prepared compounds were investigated against four bacterial strains: Xanthomonas campestris, Escherichia coli, Bacillus cereus, Bacillus megaterium, and a fungal strain Candida albicans. The biological evaluation studies of these indazole derivatives revealed that some of these tested compounds have shown moderate to goodin vitroantimicrobial activities.


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):  
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.


Author(s):  
Bindhu R. Kamath ◽  
Sabeena Kizhedath

Background: Cassia fistula Linn is a plant which is widely grown in India and is used for medicinal purposes. The study was carried out with an objective to demonstrate the antimicrobial activity of leaves of Cassia fistula Linn. The aim of the study is to assess antibacterial and antifungal activity of methanolic leaf extract of Cassia fistula Linn against selected clinical isolates.Methods: The antimicrobial activity of methanolic extract of Cassia fistula was evaluated using agar well diffusion method and to zone of inhibition of extract was determined. Clinical isolates of Staphyloccocus aureus, MRSA, Pseudomonas aeruginosa, E. coli and Proteus were screened.Results: The methanolic extracts exhibited antibacterial activity against Staphylococcus aureus. The extract was not active against E. coli, Proteus, MRSA, Pseudomonas aeruginosa. The extract also failed to demonstrate antifungal activity against Candida albicans and Aspergillus niger.Conclusions: The global emergence of multidrug resistant bacterial strains is increasing, limiting the effectiveness of current drugs and treatment failure of infections. A novel approach to the prevention of antibiotic resistance of pathogenic species is the use of new compounds that are not based on existing synthetic antimicrobial agents.


Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3959 ◽  
Author(s):  
Marc ◽  
Araniciu ◽  
Oniga ◽  
Vlase ◽  
Pîrnău ◽  
...  

 In an effort to improve the antimicrobial activity of norfloxacin, a series of hybrid norfloxacin–thiazolidinedione molecules were synthesized and screened for their direct antimicrobial activity and their anti-biofilm properties. The new hybrids were intended to have a new binding mode to DNA gyrase, that will allow for a more potent antibacterial effect, and for activity against current quinolone-resistant bacterial strains. Moreover, the thiazolidinedione moiety aimed to include additional anti-pathogenicity by preventing biofilm formation. The resulting compounds showed promising direct activity against Gram-negative strains, and anti-biofilm activity against Gram-positive strains. Docking studies and ADMET were also used in order to explain the biological properties and revealed some potential advantages over the parent molecule norfloxacin.


2011 ◽  
Vol 339 ◽  
pp. 317-320 ◽  
Author(s):  
Yu Ting Liu ◽  
Xiao Ming Sun ◽  
Da Wei Yin

A series of Ferrocene Schiff bases derived from glycine and their cobalt (II), copper (II), nickel (II), and zinc (II) metal complexes have been synthesized and characterized by IR, 1H NMR, MS and elemental analysis, the results conformed well with expected structures. The synthesized ligands, along with their metal (II) complexes, were screened in vitro for their antibacterial 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 the metal (II) complexes are more potent in antibacterial activity against one or more species in comparison with those of uncomplexed ligands.


2019 ◽  
Vol 13 (2) ◽  
pp. 120-128
Author(s):  
Amal Thebti ◽  
Ines Chniti ◽  
Med Abderrahmane Sanhoury ◽  
Ikram Chehidi ◽  
Hadda Imene Ouzari ◽  
...  

Background:The widespread occurrence of resistance to current antibiotics has triggered increasing research efforts to design and develop innovative antibacterial and antifungal agents that could overcome such antimicrobial resistance.Objective:The aim of this work was the in vitro evaluation of twelve highly fluorinated Nmonosubstituted thiocarbamates and dithiocarbamates and six non-fluorinated analogs against nine bacterial strains and three fungal species.Methods:The in vitro antimicrobial activity against the tested microrganisms was evaluated using the microdilution broth method.Results:Escherichia coli ATCC 8739, Salmonella sp., Staphylococcus aureus 6539 and all the three fungi (Aspergillus niger, Aspergillus flavus and Penicillium expansum) exhibited the highest rate of susceptibility, whilst Enterococcus faecuim ATCC 19436 and particularly Escherichia coli DH5α were less susceptible. Thiocarbamate (1i) and dithiocarbamate (2i) showed both the lowest MIC values (3.9 µg/mL) and the widest spectrum of antibacterial activity. Furthermore, the N-ethyl derivatives inhibited more efficiently the growth of bacteria than N-aryl analogs.Conclusion:The fluorinated compounds showed, in general, a relatively more potent antibacterial activity than non-fluorinated counterparts. The results indicate that these thiocarbamates and dithiocarbamates could be promising candidates as potential antimicrobial agents.


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