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

Author:

Durcik Martina1ORCID,Cotman Andrej Emanuel1ORCID,Toplak Žan1,Možina Štefan1ORCID,Skok Žiga1,Szili Petra Eva2,Czikkely Márton2,Maharramov Elvin2,Vu Thu Hien2,Piras Maria Vittoria1ORCID,Zidar Nace1ORCID,Ilaš Janez1ORCID,Zega Anamarija1ORCID,Trontelj Jurij1,Pardo Luis A.3ORCID,Hughes Diarmaid4,Huseby Douglas4ORCID,Berruga-Fernández Tália4ORCID,Cao Sha4,Simoff Ivailo5ORCID,Svensson Richard5,Korol Sergiy V.6ORCID,Jin Zhe6,Vicente Francisca7,Ramos Maria C.7ORCID,Mundy Julia E. A.8,Maxwell Anthony8ORCID,Stevenson Clare E. M.8,Lawson David M.8,Glinghammar Björn9,Sjöström Eva10,Bohlin Martin10,Oreskär Joanna10,Alvér Sofie10,Janssen Guido V.11,Sterk Geert Jan11,Kikelj Danijel1,Pal Csaba2,Tomašič Tihomir1ORCID,Peterlin Mašič Lucija1ORCID

Affiliation:

1. Faculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia

2. Synthetic and Systems Biology Unit, Institute of Biochemistry, Biological Research Centre, Szeged H-6726, Hungary

3. Max Planck Institute for Multidisciplinary Sciences, Oncophysiology, Hermann-Rein-Str. 3, Göttingen 37075, Germany

4. Department of Medical Biochemistry and Microbiology, Uppsala University, Husargatan 3, Uppsala 75123, Sweden

5. Drug Optimization and Pharmaceutical Profiling Platform (UDOPP) Department of Pharmacy, Uppsala University, Husargatan 3, Uppsala 75123, Sweden

6. Department of Medical Cell Biology, Uppsala University, Husargatan 3, Uppsala 75123, Sweden

7. Fundación Medina, Avenida del Conocimiento 34, Parque Tecnológico Ciencias de la Salud, Granada 18016, Spain

8. Department of Biochemistry and Metabolism, John Innes Centre, Norwich Research Park, Norwich NR4 7UH, U.K.

9. Department of Chemical and Pharmaceutical Toxicology, RISE Research Institutes of Sweden, Södertälje 15136, Sweden

10. Department of Chemical Processes and Pharmaceutical Development, RISE Research Institutes of Sweden, Södertälje 15136, Sweden

11. Medicinal Chemistry Division, Vrije Universiteit Amsterdam, De Boelelaan 1108, Amsterdam 1081 HZ, The Netherlands

Funder

The Wellcome Trust DBT India Alliance

Javna Agencija za Raziskovalno Dejavnost RS

National Academy of Sciences

Innovative Medicines Initiative

H2020 European Institute of Innovation and Technology

Nemzeti Kutatási Fejlesztési és Innovációs Hivatal

European Federation of Pharmaceutical Industries and Associations

Biotechnology and Biological Sciences Research Council

Seventh Framework Programme

National Laboratory of Biotechnology

ELKH Lendület Programme

Redx Pharma Plc

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Reference55 articles.

1. Keeping it simple: lessons from the golden era of antibiotic discovery

2. Where Have all the Antibiotics Gone?

3. Antimicrobial resistance. https://www.who.int/news-room/fact-sheets/detail/antimicrobial-resistance (accessed May 13, 2022).

4. O’Neill, J. Review on Antimicrobial Resistance Antimicrobial Resistance: Tackling a Crisis for the Health and Wealth of Nations. London: Review on Antimicrobial Resistance. 2014, https://amr-review.org/sites/default/files/AMR%20Review%20Paper%20-%20Tackling%20a%20crisis%20for%20the%20health%20and%20wealth%20of%20nations_1.pdf (accessed May 13, 2022).

5. Global burden of bacterial antimicrobial resistance in 2019: a systematic analysis

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