scholarly journals Novel 2,4-disubstituted quinazoline analogs as antibacterial agents with improved cytotoxicity profile: Modification of the benzenoid part

Author(s):  
Sarah H. Megahed ◽  
Sari Rasheed ◽  
Jennifer Herrmann ◽  
Ebaa M. El-Hossary ◽  
Yahia I. El-Shabrawy ◽  
...  
Planta Medica ◽  
2014 ◽  
Vol 80 (16) ◽  
Author(s):  
AC Valle ◽  
L Rabelo ◽  
AL Magalhães ◽  
M Neves ◽  
I Maciel ◽  
...  

2015 ◽  
Vol 60 (6) ◽  
pp. 511-520 ◽  
Author(s):  
A.A. Efremov ◽  
◽  
V.G. Litovchenko ◽  
V.P. Melnik ◽  
O.S. Oberemok ◽  
...  

2020 ◽  
Author(s):  
Eleonora Diamanti ◽  
Inda Setyawati ◽  
Spyridon Bousis ◽  
leticia mojas ◽  
lotteke Swier ◽  
...  

Here, we report on the virtual screening, design, synthesis and structure–activity relationships (SARs) of the first class of selective, antibacterial agents against the energy-coupling factor (ECF) transporters. The ECF transporters are a family of transmembrane proteins involved in the uptake of vitamins in a wide range of bacteria. Inhibition of the activity of these proteins could reduce the viability of pathogens that depend on vitamin uptake. Because of their central role in the metabolism of bacteria and their absence in humans, ECF transporters are novel potential antimicrobial targets to tackle infection. The hit compound’s metabolic and plasma stability, the potency (20, MIC Streptococcus pneumoniae = 2 µg/mL), the absence of cytotoxicity and a lack of resistance development under the conditions tested here suggest that this scaffold may represent a promising starting point for the development of novel antimicrobial agents with an unprecedented mechanism of action.<br>


2019 ◽  
pp. 51-53
Author(s):  
D. S. Tulanov ◽  
S. K. Dalimova ◽  
N. I. Juraeva ◽  
S. R. Mamarasulova
Keyword(s):  

2018 ◽  
Vol 22 (2) ◽  
pp. 311-317
Author(s):  
O.A. Nazarchuk ◽  
A.I. Starodub ◽  
O.V. Rymsha ◽  
V.A. Starodub ◽  
S.A. Kolodii

The study of the etiological structure, the properties of pathogens of the respiratory infectious diseases in children and their resistance to antibacterial agents is particularly relevant in modern conditions, expands the search for new approaches to combating pathogens, improves the results of treatment and reduces the mortality of this pathology. The aim — study of etiological structure, sensitivity to antibiotics and antiseptics of pathogens of infectious and inflammatory diseases of respiratory organs in children. In the study there were enrolled 247 patients who were treated in Vinnytsia Regional Children’s Clinical Hospital (VRCCH) in 2016. The sensitivity of microorganisms to 23 antibacterial agents was determined by the disc-diffusion method according to the generally accepted method. The analysis of the antimicrobial activity of antiseptic drugs (decamethoxine, miramistin, chlorhexidine digluconate) was performed by a double serial dilution technique with the determination of the minimum inhibitory bacteriostatic (MIC) and bactericidal (MBcC) concentrations, by the method of successive serial dilutions of the drug in a liquid nutrient medium. In patients who were in inpatient treatment at the VRCCH in 2016 because of pneumonia there were found opportunistic microorganisms which were of etiological significance in the development of the infection. Among them there were Streptococci (47,3 %), Staphylococci (15,3 %), Candida (13,3 %), Enterococci (10,9 %), including a high proportion of owned non-fermenting gram negative bacilli (9,8%) and species of Enterobacteria (2,0 %). Isolated strains of microorganisms had moderate resistance to most modern antibiotic drugs. The sensitivity of isolated strains of microorganisms to reserved antibiotics as carbapenems, often being used in the treatment of critical states of patients in the intensive care units, was found to above 18,2%. The sensitivity to this antibiotic in Enterococcus spp. (7,1 %), Staphylococcus spp. (5,9 %) was also low. Carbapenems, fluoroquinolones (the 1st and 2nd generations), antibiotics and aminoglycosides were found to be effective against gram positive microorganisms in more then 45% of cases. According to this they were considered to be as drugs of choice in the treatment of infectious and purulent-inflammatory pathology of respiratory organs, caused metitcilin- and vancomycin-resistant strains of microorganisms. Resistance to these drugs among investigated strains did not exceed 9,0 %. The high bactericidal properties of antiseptics as decamethoxine was determined against S.pyogenes, Staphylococcus spp. Its MBcC against these bacteria (1,65±0,20 mkg/ml and 4,32±0,50 mkg/ml, respectively) proved the advantage of decamethoxine’s effectiveness in comparison with chlorhexidine digluconate 3,14 times, 2,44 times miramistin. Clinical strains of C.albicans showed the highest susceptibility to decamethoxine, which fungicidal activity was determined in the presence (16,17±2,33 mkg/ml), in comparison with chlorxedine (MFtsK 27,59±3,59 mg/ml) and miramistin activity (27,59±3,595 mkg/ml). In children with inflammatory diseases of the respiratory organs gram-positive cocci are among the predominant pathogens (73,5 %) of cases, in the association allocated – 8,0 % of pathogens. Allocated strains of microorganisms were moderately resistant to all antibiotics studied. For antimicrobial activity antiseptic drugs, especially decamethoxine, have advantages over antibiotics confirming the possibility of their use in combination with systemic antibacterials.


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