ArticleJournal of medicinal chemistry2023
New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate
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Article in Journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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13 citing papers in PubMed.
- Antimicrobial and Antibiofilm Activities of Glycyl-Histidine and Methionyl-Glycine Dipeptides: In Vitro and Molecular Docking Studies.Molecules (Basel, Switzerland) · 2026Article
- Synthesis and antibacterial evaluation of trisindolines against methicillin-resistant Staphylococcus aureus targeting cell membrane.NPJ biofilms and microbiomes · 2025Article
- Recent advancements in the development of next-generation dual-targeting antibacterial agents.RSC medicinal chemistry · 2025Review
- Intranasal Galanin (1-15) modulates alcohol self-administration and depressive-like behavior in rats and shows a favorable safety profile.Frontiers in pharmacology · 2025Article
- Methyl 2-amino-4-(morpholin-4-yl)benzo[IUCrData · 2025Article
- Emerging Antimicrobial Strategies Against Heterogeneous and Vancomycin-IntermediateInternational journal of general medicine · 2025Review
- Hiding in plain sight: Optimizing topoisomerase IIα inhibitors into Hsp90β selective binders.European journal of medicinal chemistry · 2024Article
- Unlocking the Potential of Pyrrole: Recent Advances in New Pyrrole-Containing Compounds with Antibacterial Potential.International journal of molecular sciences · 2024Review
- Enhancing Antibacterial Efficacy: Combining Novel Bacterial Topoisomerase Inhibitors with Efflux Pump Inhibitors and Other Agents Against Gram-Negative Bacteria.Antibiotics (Basel, Switzerland) · 2024Article
- NewRSC advances · 2024Article
- Benzothiazole DNA gyrase inhibitors and their conjugates with siderophore mimics: design, synthesis and evaluation.RSC advances · 2024Article
- Exploring the 5-Substituted 2-Aminobenzothiazole-Based DNA Gyrase B Inhibitors Active against ESKAPE Pathogens.ACS omega · 2023Article
- An Update Review of Approaches to Multiple Action-Based Antibacterials.Antibiotics (Basel, Switzerland) · 2023Review
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Authors and funding
40 authors.
Martina DurcikFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia.ORCID 0000-0002-9218-1771
Andrej Emanuel CotmanFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia.ORCID 0000-0003-2528-396X
Žan ToplakFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia.
Štefan MožinaFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia.ORCID 0000-0002-7416-6981
Žiga SkokFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia.
Petra Eva SziliSynthetic and Systems Biology Unit, Institute of Biochemistry, Biological Research Centre, Szeged H-6726, Hungary.
Márton CzikkelySynthetic and Systems Biology Unit, Institute of Biochemistry, Biological Research Centre, Szeged H-6726, Hungary.
Elvin MaharramovSynthetic and Systems Biology Unit, Institute of Biochemistry, Biological Research Centre, Szeged H-6726, Hungary.
Thu Hien VuSynthetic and Systems Biology Unit, Institute of Biochemistry, Biological Research Centre, Szeged H-6726, Hungary.
Maria Vittoria PirasFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia.ORCID 0000-0002-0663-3373
Nace ZidarFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia.ORCID 0000-0003-1905-0158
Janez IlašFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia.ORCID 0000-0002-0124-0474
Anamarija ZegaFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia.ORCID 0000-0003-4065-0019
Jurij TronteljFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia.
Luis A PardoMax Planck Institute for Multidisciplinary Sciences, Oncophysiology, Hermann-Rein-Str. 3, Göttingen 37075, Germany.ORCID 0000-0003-1375-4349
Diarmaid HughesDepartment of Medical Biochemistry and Microbiology, Uppsala University, Husargatan 3, Uppsala 75123, Sweden.
Douglas HusebyDepartment of Medical Biochemistry and Microbiology, Uppsala University, Husargatan 3, Uppsala 75123, Sweden.ORCID 0000-0001-9974-578X
Tália Berruga-FernándezDepartment of Medical Biochemistry and Microbiology, Uppsala University, Husargatan 3, Uppsala 75123, Sweden.ORCID 0000-0001-6459-1397
Sha CaoDepartment of Medical Biochemistry and Microbiology, Uppsala University, Husargatan 3, Uppsala 75123, Sweden.
Ivailo SimoffDrug Optimization and Pharmaceutical Profiling Platform (UDOPP) Department of Pharmacy, Uppsala University, Husargatan 3, Uppsala 75123, Sweden.ORCID 0000-0001-6522-7191
Richard SvenssonDrug Optimization and Pharmaceutical Profiling Platform (UDOPP) Department of Pharmacy, Uppsala University, Husargatan 3, Uppsala 75123, Sweden.
Sergiy V KorolDepartment of Medical Cell Biology, Uppsala University, Husargatan 3, Uppsala 75123, Sweden.ORCID 0000-0001-8279-2790
Zhe JinDepartment of Medical Cell Biology, Uppsala University, Husargatan 3, Uppsala 75123, Sweden.
Francisca VicenteFundación Medina, Avenida del Conocimiento 34, Parque Tecnológico Ciencias de la Salud, Granada 18016, Spain.
Maria C RamosFundación Medina, Avenida del Conocimiento 34, Parque Tecnológico Ciencias de la Salud, Granada 18016, Spain.ORCID 0000-0002-3674-615X
Julia E A MundyDepartment of Biochemistry and Metabolism, John Innes Centre, Norwich Research Park, Norwich NR4 7UH, U.K.
Anthony MaxwellDepartment of Biochemistry and Metabolism, John Innes Centre, Norwich Research Park, Norwich NR4 7UH, U.K.ORCID 0000-0002-5756-6430
Clare E M StevensonDepartment of Biochemistry and Metabolism, John Innes Centre, Norwich Research Park, Norwich NR4 7UH, U.K.
David M LawsonDepartment of Biochemistry and Metabolism, John Innes Centre, Norwich Research Park, Norwich NR4 7UH, U.K.
Björn GlinghammarDepartment of Chemical and Pharmaceutical Toxicology, RISE Research Institutes of Sweden, Södertälje 15136, Sweden.
Eva SjöströmDepartment of Chemical Processes and Pharmaceutical Development, RISE Research Institutes of Sweden, Södertälje 15136, Sweden.
Martin BohlinDepartment of Chemical Processes and Pharmaceutical Development, RISE Research Institutes of Sweden, Södertälje 15136, Sweden.
Joanna OreskärDepartment of Chemical Processes and Pharmaceutical Development, RISE Research Institutes of Sweden, Södertälje 15136, Sweden.
Sofie AlvérDepartment of Chemical Processes and Pharmaceutical Development, RISE Research Institutes of Sweden, Södertälje 15136, Sweden.
Guido V JanssenMedicinal Chemistry Division, Vrije Universiteit Amsterdam, De Boelelaan 1108, Amsterdam 1081 HZ, The Netherlands.
Geert Jan SterkMedicinal Chemistry Division, Vrije Universiteit Amsterdam, De Boelelaan 1108, Amsterdam 1081 HZ, The Netherlands.
Danijel KikeljFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia.
Csaba PalSynthetic and Systems Biology Unit, Institute of Biochemistry, Biological Research Centre, Szeged H-6726, Hungary.
Tihomir TomašičFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia.ORCID 0000-0001-5534-209X
Lucija Peterlin MašičFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, Ljubljana 1000, Slovenia.ORCID 0000-0003-0624-8472
Funding
Biotechnology and Biological Sciences Research Council BB/J014524/1Biotechnology and Biological Sciences Research Council BB/P012523/1Wellcome TrustWellcome Trust 110072/Z/15/Z
Abstract
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
Indexed as
Staphylococcus aureusVancomycin-Resistant Staphylococcus aureusAnimalsAnti-Bacterial AgentsDNA GyraseDNA Topoisomerase IVMiceMicrobial Sensitivity TestsAnti-Bacterial AgentsDNA GyraseDNA Topoisomerase IV
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.