TY  - JOUR
AU  - Shetnev, Anton
AU  - Tarasenko, Marina
AU  - Kotlyarova, Valentina
AU  - Baykov, Sergey
AU  - Geyl, Kirill
AU  - Kasatkina, Svetlana
AU  - Sibinčić, Nikolina
AU  - Sharoyko, Vladimir
AU  - Rogacheva, Elizaveta
AU  - Kraeva, Liudmila
PY  - 2022
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/6050
AB  - A new route to 5-amino-1,2,4-thiadiazole derivatives via reaction of N-chloroamidines with isothiocyanates has been proposed. The advantages of this method are high product yields (up to 93%), the column chromatography-free workup procedure, scalability and the absence of additive oxidizing agents or transition metal catalysts. The 28 examples of 5-amino-1,2,4thiadiazole derivatives obtaining via the proposing protocol were evaluated in vitro against ESKAPE pathogens strains (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter cloacae). It was found that compounds 5ba, 5bd, 6a, 6d and 6c have potent antibacterial activity (MIC values 0.09–1.5 μg mL−1), which is superior to the activity of commercial antibiotics such as pefloxacin (MIC 4–8 μg  mL−1) and streptomycin (MIC 2–32 μg  mL−1). The additional cytotoxic assay of hit compounds on PANC-1 cell line demonstrated the low or non-cytotoxicity activity at the same level of concentrations. Thus, these 5 compounds are promising starting point for further antimicrobial drug development.
PB  - Springer
T2  - Molecular Diversity
T1  - External oxidant‐free and transition metal‐free synthesis of 5‐amino‐1,2,4‐thiadiazoles as promising antibacterials against ESKAPE pathogen strains
VL  - 27
SP  - 651
EP  - 666
DO  - 10.1007/s11030-022-10445-1
ER  - 

@article{
author = "Shetnev, Anton and Tarasenko, Marina and Kotlyarova, Valentina and Baykov, Sergey and Geyl, Kirill and Kasatkina, Svetlana and Sibinčić, Nikolina and Sharoyko, Vladimir and Rogacheva, Elizaveta and Kraeva, Liudmila",
year = "2022",
abstract = "A new route to 5-amino-1,2,4-thiadiazole derivatives via reaction of N-chloroamidines with isothiocyanates has been proposed. The advantages of this method are high product yields (up to 93%), the column chromatography-free workup procedure, scalability and the absence of additive oxidizing agents or transition metal catalysts. The 28 examples of 5-amino-1,2,4thiadiazole derivatives obtaining via the proposing protocol were evaluated in vitro against ESKAPE pathogens strains (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter cloacae). It was found that compounds 5ba, 5bd, 6a, 6d and 6c have potent antibacterial activity (MIC values 0.09–1.5 μg mL−1), which is superior to the activity of commercial antibiotics such as pefloxacin (MIC 4–8 μg  mL−1) and streptomycin (MIC 2–32 μg  mL−1). The additional cytotoxic assay of hit compounds on PANC-1 cell line demonstrated the low or non-cytotoxicity activity at the same level of concentrations. Thus, these 5 compounds are promising starting point for further antimicrobial drug development.",
publisher = "Springer",
journal = "Molecular Diversity",
title = "External oxidant‐free and transition metal‐free synthesis of 5‐amino‐1,2,4‐thiadiazoles as promising antibacterials against ESKAPE pathogen strains",
volume = "27",
pages = "651-666",
doi = "10.1007/s11030-022-10445-1"
}

Shetnev, A., Tarasenko, M., Kotlyarova, V., Baykov, S., Geyl, K., Kasatkina, S., Sibinčić, N., Sharoyko, V., Rogacheva, E.,& Kraeva, L.. (2022). External oxidant‐free and transition metal‐free synthesis of 5‐amino‐1,2,4‐thiadiazoles as promising antibacterials against ESKAPE pathogen strains. in Molecular Diversity
Springer., 27, 651-666.
https://doi.org/10.1007/s11030-022-10445-1

Shetnev A, Tarasenko M, Kotlyarova V, Baykov S, Geyl K, Kasatkina S, Sibinčić N, Sharoyko V, Rogacheva E, Kraeva L. External oxidant‐free and transition metal‐free synthesis of 5‐amino‐1,2,4‐thiadiazoles as promising antibacterials against ESKAPE pathogen strains. in Molecular Diversity. 2022;27:651-666.
doi:10.1007/s11030-022-10445-1 .

Shetnev, Anton, Tarasenko, Marina, Kotlyarova, Valentina, Baykov, Sergey, Geyl, Kirill, Kasatkina, Svetlana, Sibinčić, Nikolina, Sharoyko, Vladimir, Rogacheva, Elizaveta, Kraeva, Liudmila, "External oxidant‐free and transition metal‐free synthesis of 5‐amino‐1,2,4‐thiadiazoles as promising antibacterials against ESKAPE pathogen strains" in Molecular Diversity, 27 (2022):651-666,
https://doi.org/10.1007/s11030-022-10445-1 . .