New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate Staphylococcus aureus

Autor: Martina Durcik, Andrej Emanuel Cotman, Žan Toplak, Štefan Možina, Žiga Skok, Petra Eva Szili, Márton Czikkely, Elvin Maharramov, Thu Hien Vu, Maria Vittoria Piras, Nace Zidar, Janez Ilaš, Anamarija Zega, Jurij Trontelj, Luis A. Pardo, Diarmaid Hughes, Douglas Huseby, Tália Berruga-Fernández, Sha Cao, Ivailo Simoff, Richard Svensson, Sergiy V. Korol, Zhe Jin, Francisca Vicente, Maria C. Ramos, Julia E. A. Mundy, Anthony Maxwell, Clare E. M. Stevenson, David M. Lawson, Björn Glinghammar, Eva Sjöström, Martin Bohlin, Joanna Oreskär, Sofie Alvér, Guido V. Janssen, Geert Jan Sterk, Danijel Kikelj, Csaba Pal, Tihomir Tomašič, Lucija Peterlin Mašič

Publikováno v: Durcik, M, Cotman, A E, Toplak, Ž, Možina, Š, Skok, Ž, Szili, P E, Czikkely, M, Maharramov, E, Vu, T H, Piras, M V, Zidar, N, Ilaš, J, Zega, A, Trontelj, J, Pardo, L A, Hughes, D, Huseby, D, Berruga-Fernández, T, Cao, S, Simoff, I, Svensson, R, Korol, S V, Jin, Z, Vicente, F, Ramos, M C, Mundy, J E A, Maxwell, A, Stevenson, C E M, Lawson, D M, Glinghammar, B, Sjöström, E, Bohlin, M, Oreskär, J, Alvér, S, Janssen, G V, Sterk, G J, Kikelj, D, Pal, C, Tomašič, T & Peterlin Mašič, L 2023, ' New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate Staphylococcus aureus ', Journal of medicinal chemistry, vol. 66, no. 6, pp. 3968-3994 . https://doi.org/10.1021/acs.jmedchem.2c01905
Journal of medicinal chemistry, 66(6), 3968-3994. American Chemical Society
Journal of Medicinal Chemistry
Journal of medicinal chemistry, str. 3968-3994 : Ilustr., Vol. 66, iss. 6, 2023
COBISS-ID: 512806681
Journal of medicinal chemistry, vol. 66, no. 6, pp. 3968-3994, 2023.

A new series of dual low nanomolar benzothiazole inhibitors of bacterial DNA gyrase and topoisomerase IV were developed. The resulting compounds show excellent broad-spectrum antibacterial activities against Gram-positive Enterococcus faecalis, Enter

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::55c3d01f7594899ad1504d0f95893f77
http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-501871

Računalniška analiza primernosti encima MurC za načrtovanje novih protibakterijskih učinkovin

Autor: Černe, Anja

Bakterijska odpornost na trenutno dostopna antibiotična zdravila je eden največjih problemov javnega zdravja. K njenemu pojavu prispevata neustrezna in/ali prekomerna uporaba antibiotikov ter upadel razvoj novih antibiotičnih zdravil v zadnjih let

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=od______3505::faa33f5cad3a7dcbc206a21ea9957e04
https://repozitorij.uni-lj.si/IzpisGradiva.php?id=144329

Discovery of a fragment hit compound targeting D-Ala

Autor: Proj, Matic, Hrast, Martina, Bajc, Gregor, dipl biol, Frlan, Rok, Meden, Anže, Butala, Matej, biokemik, Gobec, Stanislav

Publikováno v: Journal of enzyme inhibition and medicinal chemistry, vol. 38, no. 11, pp. 387-397, 2023.
Journal of enzyme inhibition and medicinal chemistry, str. 387-397 : Ilustr., Vol. 38, iss. 1, 2023
COBISS-ID: 22763225

Bacterial resistance is an increasing threat to healthcare systems, highlighting the need for discovering new antibacterial agents. An established technique, fragment-based drug discovery, was used to target a bacterial enzyme Ddl involved in the bio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=dedup_wf_001::785471e52d8f9c46a5a6594fdb08ec69
https://repozitorij.uni-lj.si/Dokument.php?id=164549&dn=

The structural features of novel bacterial topoisomerase inhibitors that define their activity on topoisomerase IV

Autor: Maja Kokot, Marko Anderluh, Martina Hrast, Nikola Minovski

Publikováno v: Journal of medicinal chemistry, vol. 65, no. 9, 2022.

The continued emergence of bacterial resistance has created an urgent need for new and effective antibacterial agents. Bacterial type II topoisomerases, such as DNA gyrase and topoisomerase IV (topoIV), are well-validated targets for antibacterial ch

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56f1f38addb8c66101daba9d353640fa
https://repozitorij.uni-lj.si/Dokument.php?id=162061&dn=

Hybrid inhibitors of DNA gyrase A and B

Autor: Durcik, Martina, Skok, Žiga, Ilaš, Janez, Zidar, Nace, Zega, Anamarija, Szili, Petra, Draskovits, Gábor, Revesz, T., Kikelj, Danijel, Nyerges, Ákos, Pál, Csaba, Peterlin-Mašič, Lucija, Tomašič, Tihomir

Publikováno v: Pharmaceutics, vol. 13, no. 1, 6, 2021.

The discovery of multi-targeting ligands of bacterial enzymes is an important strategy to combat rapidly spreading antimicrobial resistance. Bacterial DNA gyrase and topoisomerase IV are validated targets for the development of antibiotics. They can

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=od______3505::74e67012ba0d67e86a690c2e0f91e467
https://repozitorij.uni-lj.si/Dokument.php?id=153416&dn=