2020
DOI: 10.3390/molecules26010170
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Antibacterial Activity of Fluorobenzoylthiosemicarbazides and Their Cyclic Analogues with 1,2,4-Triazole Scaffold

Abstract: The development of drug-resistant bacteria is currently one of the major challenges in medicine. Therefore, the discovery of novel lead structures for the design of antibacterial drugs is urgently needed. In this structure–activity relationship study, a library of ortho-, meta-, and para-fluorobenzoylthiosemicarbazides, and their cyclic analogues with 1,2,4-triazole scaffold, was created and tested for antibacterial activity against Gram-positive bacteria strains. While all tested 1,2,4-triazoles were devoid o… Show more

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Cited by 27 publications
(15 citation statements)
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“…Moreover, the lack of the antibacterial activity against P. aeruginosa and P. gingivalis demonstrate that our system is highly selective in killing different strains of bacteria, and this can be considered an important advantage. Concerning the molecular mechanism of the antibacterial activity of these types of compounds, it is still under debate in the literature, but it seems that the inhibitory action towards bacterial topoisomerases could be the main explanation [ 37 , 38 ]. Undoubtedly, more in-depth research in this area is urgently needed in order to establish the exact mechanism of action of these compounds.…”
Section: Resultsmentioning
confidence: 99%
“…Moreover, the lack of the antibacterial activity against P. aeruginosa and P. gingivalis demonstrate that our system is highly selective in killing different strains of bacteria, and this can be considered an important advantage. Concerning the molecular mechanism of the antibacterial activity of these types of compounds, it is still under debate in the literature, but it seems that the inhibitory action towards bacterial topoisomerases could be the main explanation [ 37 , 38 ]. Undoubtedly, more in-depth research in this area is urgently needed in order to establish the exact mechanism of action of these compounds.…”
Section: Resultsmentioning
confidence: 99%
“…Kosikowska and coworkers reported fluorinated 1,2,4-triazole analogs scaffold 126–131 ( Supplementary Table S1 ) ( Kosikowska et al, 2020 ). In vitro antibacterial activity was performed using six reference Gram-positive strains, eight MSSA clinical isolates, and eight MRSA clinical isolates.…”
Section: Introductionmentioning
confidence: 99%
“…However, there is still a requirement for application in industrial expert and a widely approach to the integration of zinc nanoparticles. Numerous techniques applied, for example, the combination of zinc nanoparticles, the reaction of substances and the reaction of compounds changing micelles, the extensively used of zinc oxide in radiation [ 9 , 10 , 11 , 12 ], the electrochemical, sonochemical, microwave [ 13 , 14 , 15 ] and green science applications [ 16 , 17 , 18 ].…”
Section: Introductionmentioning
confidence: 99%