TY  - JOUR
AU  - Ferjančić, Zorana
AU  - Bihelović, Filip
AU  - Vulović, Bojan
AU  - Matović, Radomir
AU  - Trmčić, Milena
AU  - Janković, Aleksandar
AU  - Pavlović, Miloš
AU  - Đurković, Filip T.
AU  - Prodanović, Radivoje
AU  - Đurđević Đelmaš, Aleksandra
AU  - Kaličanin, Nevena
AU  - Zlatović, Mario
AU  - Sladić, Dušan
AU  - Vallet, Thomas
AU  - Vignuzzi, Marco
AU  - Saičić, Radomir N.
PY  - 2024
UR  - https://cer.ihtm.bg.ac.rs/handle/123456789/7585
AB  - We developed new iminosugar-based glycosidase inhibitors against SARS-CoV-2. Known drugs (miglustat, migalastat, miglitol, and swainsonine) were chosen as lead compounds to develop three classes of glycosidase inhibitors (α-glucosidase, α-galactosidase, and mannosidase). Molecular modelling of the lead compounds, synthesis of the compounds with the highest docking scores, enzyme inhibition tests, and in vitro antiviral assays afforded rationally designed inhibitors. Two highly active α-glucosidase inhibitors were discovered, where one of them is the most potent iminosugar-based anti-SARS-CoV-2 agent to date (EC90 = 1.94 µM in A549-ACE2 cells against Omicron BA.1 strain). However, galactosidase inhibitors did not exhibit antiviral activity, whereas mannosidase inhibitors were both active and cytotoxic. As our iminosugar-based drug candidates act by a host-directed mechanism, they should be more resilient to drug resistance. Moreover, this strategy could be extended to identify potential drug candidates for other viral infections.
PB  - Taylor and Francis Group
T2  - Journal of Enzyme Inhibition and Medicinal Chemistry
T1  - Development of iminosugar-based glycosidase inhibitors as drug candidates for SARS-CoV-2 virus via molecular modelling and in vitro studies
VL  - 39
IS  - 1
SP  - 2289007
DO  - 10.1080/14756366.2023.2289007
ER  - 

@article{
author = "Ferjančić, Zorana and Bihelović, Filip and Vulović, Bojan and Matović, Radomir and Trmčić, Milena and Janković, Aleksandar and Pavlović, Miloš and Đurković, Filip T. and Prodanović, Radivoje and Đurđević Đelmaš, Aleksandra and Kaličanin, Nevena and Zlatović, Mario and Sladić, Dušan and Vallet, Thomas and Vignuzzi, Marco and Saičić, Radomir N.",
year = "2024",
abstract = "We developed new iminosugar-based glycosidase inhibitors against SARS-CoV-2. Known drugs (miglustat, migalastat, miglitol, and swainsonine) were chosen as lead compounds to develop three classes of glycosidase inhibitors (α-glucosidase, α-galactosidase, and mannosidase). Molecular modelling of the lead compounds, synthesis of the compounds with the highest docking scores, enzyme inhibition tests, and in vitro antiviral assays afforded rationally designed inhibitors. Two highly active α-glucosidase inhibitors were discovered, where one of them is the most potent iminosugar-based anti-SARS-CoV-2 agent to date (EC90 = 1.94 µM in A549-ACE2 cells against Omicron BA.1 strain). However, galactosidase inhibitors did not exhibit antiviral activity, whereas mannosidase inhibitors were both active and cytotoxic. As our iminosugar-based drug candidates act by a host-directed mechanism, they should be more resilient to drug resistance. Moreover, this strategy could be extended to identify potential drug candidates for other viral infections.",
publisher = "Taylor and Francis Group",
journal = "Journal of Enzyme Inhibition and Medicinal Chemistry",
title = "Development of iminosugar-based glycosidase inhibitors as drug candidates for SARS-CoV-2 virus via molecular modelling and in vitro studies",
volume = "39",
number = "1",
pages = "2289007",
doi = "10.1080/14756366.2023.2289007"
}

Ferjančić, Z., Bihelović, F., Vulović, B., Matović, R., Trmčić, M., Janković, A., Pavlović, M., Đurković, F. T., Prodanović, R., Đurđević Đelmaš, A., Kaličanin, N., Zlatović, M., Sladić, D., Vallet, T., Vignuzzi, M.,& Saičić, R. N.. (2024). Development of iminosugar-based glycosidase inhibitors as drug candidates for SARS-CoV-2 virus via molecular modelling and in vitro studies. in Journal of Enzyme Inhibition and Medicinal Chemistry
Taylor and Francis Group., 39(1), 2289007.
https://doi.org/10.1080/14756366.2023.2289007

Ferjančić Z, Bihelović F, Vulović B, Matović R, Trmčić M, Janković A, Pavlović M, Đurković FT, Prodanović R, Đurđević Đelmaš A, Kaličanin N, Zlatović M, Sladić D, Vallet T, Vignuzzi M, Saičić RN. Development of iminosugar-based glycosidase inhibitors as drug candidates for SARS-CoV-2 virus via molecular modelling and in vitro studies. in Journal of Enzyme Inhibition and Medicinal Chemistry. 2024;39(1):2289007.
doi:10.1080/14756366.2023.2289007 .

Ferjančić, Zorana, Bihelović, Filip, Vulović, Bojan, Matović, Radomir, Trmčić, Milena, Janković, Aleksandar, Pavlović, Miloš, Đurković, Filip T., Prodanović, Radivoje, Đurđević Đelmaš, Aleksandra, Kaličanin, Nevena, Zlatović, Mario, Sladić, Dušan, Vallet, Thomas, Vignuzzi, Marco, Saičić, Radomir N., "Development of iminosugar-based glycosidase inhibitors as drug candidates for SARS-CoV-2 virus via molecular modelling and in vitro studies" in Journal of Enzyme Inhibition and Medicinal Chemistry, 39, no. 1 (2024):2289007,
https://doi.org/10.1080/14756366.2023.2289007 . .

TY  - JOUR
AU  - Stjepanovic, Mihailo
AU  - Janković, Aleksandar
AU  - Vulović, Bojan
AU  - Matović, Radomir
AU  - Saičić, Radomir
PY  - 2023
UR  - https://cer.ihtm.bg.ac.rs/handle/123456789/7160
AB  - The synthesis of an angular triquinane, which could serve as a suit­able platform for the synthesis of several natural products (panaginsene, sil­phi­nene, senoxydene) is described. The synthesis is based on two consecutive cyc­lo­pentene annulations, where alkenes were used as latent carbonyl function­alities (via Wacker reaction), and cyclopentenone annulation was effected by aldol condensation.
PB  - Serbian Chemical Society
T2  - Journal of the Serbian Chemical Society
T1  - Synthetic study on the angular triquinanes: Scientific paper
VL  - 88
IS  - 10
SP  - 975
EP  - 983
DO  - 10.2298/JSC230627046S
ER  - 

@article{
author = "Stjepanovic, Mihailo and Janković, Aleksandar and Vulović, Bojan and Matović, Radomir and Saičić, Radomir",
year = "2023",
abstract = "The synthesis of an angular triquinane, which could serve as a suit­able platform for the synthesis of several natural products (panaginsene, sil­phi­nene, senoxydene) is described. The synthesis is based on two consecutive cyc­lo­pentene annulations, where alkenes were used as latent carbonyl function­alities (via Wacker reaction), and cyclopentenone annulation was effected by aldol condensation.",
publisher = "Serbian Chemical Society",
journal = "Journal of the Serbian Chemical Society",
title = "Synthetic study on the angular triquinanes: Scientific paper",
volume = "88",
number = "10",
pages = "975-983",
doi = "10.2298/JSC230627046S"
}

Stjepanovic, M., Janković, A., Vulović, B., Matović, R.,& Saičić, R.. (2023). Synthetic study on the angular triquinanes: Scientific paper. in Journal of the Serbian Chemical Society
Serbian Chemical Society., 88(10), 975-983.
https://doi.org/10.2298/JSC230627046S

Stjepanovic M, Janković A, Vulović B, Matović R, Saičić R. Synthetic study on the angular triquinanes: Scientific paper. in Journal of the Serbian Chemical Society. 2023;88(10):975-983.
doi:10.2298/JSC230627046S .

Stjepanovic, Mihailo, Janković, Aleksandar, Vulović, Bojan, Matović, Radomir, Saičić, Radomir, "Synthetic study on the angular triquinanes: Scientific paper" in Journal of the Serbian Chemical Society, 88, no. 10 (2023):975-983,
https://doi.org/10.2298/JSC230627046S . .