TY  - JOUR
AU  - Kamoutsis, Charalampos
AU  - Fesatidou, Maria
AU  - Petrou, Anthi
AU  - Geronikaki, Athina
AU  - Poroikov, Vladimir
AU  - Ivanov, Marija
AU  - Soković, Marina
AU  - Ćirić, Ana
AU  - Carazo, Alejandro
AU  - Mladenka, Premysl
PY  - 2021
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/4298
AB  - The goal of this research is to investigate the antimicrobial activity of nineteen previously
synthesized 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole derivatives. The compounds were
tested against a panel of three Gram-positive and three Gram-negative bacteria, three resistant strains,
and six fungi. Minimal inhibitory, bactericidal, and fungicidal concentrations were determined by a
microdilution method. All of the compounds showed antibacterial activity that was more potent
than both reference drugs, ampicillin and streptomycin, against all bacteria tested. Similarly, they
were also more active against resistant bacterial strains. The antifungal activity of the compounds
was up to 80-fold higher than ketoconazole and from 3 to 40 times higher than bifonazole, both of
which were used as reference drugs. The most active compounds (2, 3, 6, 7, and 19) were tested for
their inhibition of P. aeruginosa biofilm formation. Among them, compound 3 showed significantly
higher antibiofilm activity and appeared to be equipotent with ampicillin. The prediction of the
probable mechanism by docking on antibacterial targets revealed that E. coli MurB is the most suitable
enzyme, while docking studies on antifungal targets indicated a probable involvement of CYP51 in
the mechanism of antifungal activity. Finally, the toxicity testing in human cells confirmed their low
toxicity both in cancerous cell line MCF7 and non-cancerous cell line HK-2.
PB  - MDPI
T2  - Antibiotics
T1  - Triazolo Based-Thiadiazole Derivatives. Synthesis, Biological Evaluation and Molecular Docking Studies
IS  - 7
VL  - 10
DO  - 10.3390/antibiotics10070804
SP  - 804
ER  - 

@article{
author = "Kamoutsis, Charalampos and Fesatidou, Maria and Petrou, Anthi and Geronikaki, Athina and Poroikov, Vladimir and Ivanov, Marija and Soković, Marina and Ćirić, Ana and Carazo, Alejandro and Mladenka, Premysl",
year = "2021",
abstract = "The goal of this research is to investigate the antimicrobial activity of nineteen previously
synthesized 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole derivatives. The compounds were
tested against a panel of three Gram-positive and three Gram-negative bacteria, three resistant strains,
and six fungi. Minimal inhibitory, bactericidal, and fungicidal concentrations were determined by a
microdilution method. All of the compounds showed antibacterial activity that was more potent
than both reference drugs, ampicillin and streptomycin, against all bacteria tested. Similarly, they
were also more active against resistant bacterial strains. The antifungal activity of the compounds
was up to 80-fold higher than ketoconazole and from 3 to 40 times higher than bifonazole, both of
which were used as reference drugs. The most active compounds (2, 3, 6, 7, and 19) were tested for
their inhibition of P. aeruginosa biofilm formation. Among them, compound 3 showed significantly
higher antibiofilm activity and appeared to be equipotent with ampicillin. The prediction of the
probable mechanism by docking on antibacterial targets revealed that E. coli MurB is the most suitable
enzyme, while docking studies on antifungal targets indicated a probable involvement of CYP51 in
the mechanism of antifungal activity. Finally, the toxicity testing in human cells confirmed their low
toxicity both in cancerous cell line MCF7 and non-cancerous cell line HK-2.",
publisher = "MDPI",
journal = "Antibiotics",
title = "Triazolo Based-Thiadiazole Derivatives. Synthesis, Biological Evaluation and Molecular Docking Studies",
number = "7",
volume = "10",
doi = "10.3390/antibiotics10070804",
pages = "804"
}

Kamoutsis, C., Fesatidou, M., Petrou, A., Geronikaki, A., Poroikov, V., Ivanov, M., Soković, M., Ćirić, A., Carazo, A.,& Mladenka, P.. (2021). Triazolo Based-Thiadiazole Derivatives. Synthesis, Biological Evaluation and Molecular Docking Studies. in Antibiotics
MDPI., 10(7), 804.
https://doi.org/10.3390/antibiotics10070804

Kamoutsis C, Fesatidou M, Petrou A, Geronikaki A, Poroikov V, Ivanov M, Soković M, Ćirić A, Carazo A, Mladenka P. Triazolo Based-Thiadiazole Derivatives. Synthesis, Biological Evaluation and Molecular Docking Studies. in Antibiotics. 2021;10(7):804.
doi:10.3390/antibiotics10070804 .

Kamoutsis, Charalampos, Fesatidou, Maria, Petrou, Anthi, Geronikaki, Athina, Poroikov, Vladimir, Ivanov, Marija, Soković, Marina, Ćirić, Ana, Carazo, Alejandro, Mladenka, Premysl, "Triazolo Based-Thiadiazole Derivatives. Synthesis, Biological Evaluation and Molecular Docking Studies" in Antibiotics, 10, no. 7 (2021):804,
https://doi.org/10.3390/antibiotics10070804 . .