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


Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
23 03 2023
Historique:
pubmed: 7 3 2023
medline: 25 3 2023
entrez: 6 3 2023
Statut: ppublish

Résumé

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

Identifiants

pubmed: 36877255
doi: 10.1021/acs.jmedchem.2c01905
pmc: PMC10041525
doi:

Substances chimiques

Anti-Bacterial Agents 0
DNA Gyrase EC 5.99.1.3
DNA Topoisomerase IV EC 5.99.1.-

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

3968-3994

Subventions

Organisme : Biotechnology and Biological Sciences Research Council
ID : BB/J014524/1
Pays : United Kingdom
Organisme : Wellcome Trust
ID : 110072/Z/15/Z
Pays : United Kingdom
Organisme : Biotechnology and Biological Sciences Research Council
ID : BB/P012523/1
Pays : United Kingdom

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Auteurs

Martina Durcik (M)

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

Andrej Emanuel Cotman (AE)

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

Žan Toplak (Ž)

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

Štefan Možina (Š)

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

Žiga Skok (Ž)

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

Petra Eva Szili (PE)

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

Márton Czikkely (M)

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

Elvin Maharramov (E)

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

Thu Hien Vu (TH)

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

Maria Vittoria Piras (MV)

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

Nace Zidar (N)

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

Janez Ilaš (J)

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

Anamarija Zega (A)

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

Jurij Trontelj (J)

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

Luis A Pardo (LA)

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

Diarmaid Hughes (D)

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

Douglas Huseby (D)

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

Tália Berruga-Fernández (T)

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

Sha Cao (S)

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

Ivailo Simoff (I)

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

Richard Svensson (R)

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

Sergiy V Korol (SV)

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

Zhe Jin (Z)

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

Francisca Vicente (F)

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

Maria C Ramos (MC)

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

Julia E A Mundy (JEA)

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

Anthony Maxwell (A)

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

Clare E M Stevenson (CEM)

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

David M Lawson (DM)

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

Björn Glinghammar (B)

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

Eva Sjöström (E)

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

Martin Bohlin (M)

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

Joanna Oreskär (J)

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

Sofie Alvér (S)

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

Guido V Janssen (GV)

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

Geert Jan Sterk (GJ)

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

Danijel Kikelj (D)

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

Csaba Pal (C)

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

Tihomir Tomašič (T)

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

Lucija Peterlin Mašič (L)

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

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Classifications MeSH