ArticleJournal of medicinal chemistry2023
Discovery and Hit-to-Lead Optimization of Benzothiazole Scaffold-Based DNA Gyrase Inhibitors with Potent Activity against
Open access · hybridAbstract read
In one paragraph
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 20 papers.
0numbers the graph read from it
0cells of the map it votes in
20citing papers in PubMed
7.8field-weighted citation impact, top 2% of its field
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
20 citing papers in PubMed, 51 citations in OpenAlex.
- GC-MS profiling and antivirulence potential of limonene-rich Citrus medica cv. 'Rugosa' essential oil: in vitro and in silico evaluations.Scientific reports · 2026Article
- Synthesis, characterization, andFrontiers in chemistry · 2026Article
- Biofilm structure as a key factor in antibiotic tolerance: insights from Bacillus subtilis model systems.NPJ biofilms and microbiomes · 2025Article
- Enhanced antibacterial and antioxidant capabilities using indole-modified 1-phenyl-1RSC advances · 2025Article
- Antimicrobial and Antibiofilm Activities of Some Antioxidant 3,4-Dihydroxyphenyl-Thiazole-Coumarin Hybrid Compounds: In Silico and In Vitro Evaluation.Antibiotics (Basel, Switzerland) · 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
- Biological Evaluation and Computational Modelling Studies onCurrent pharmaceutical design · 2025Article
- Effect of Fluorine Atoms and Piperazine Rings on Biotoxicity of Norfloxacin Analogues: Combined Experimental and Theoretical Study.Environment & health (Washington, D.C.) · 2024Article
- Hiding in plain sight: Optimizing topoisomerase IIα inhibitors into Hsp90β selective binders.European journal of medicinal chemistry · 2024Article
- 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
- AlphaFold accelerated discovery of psychotropic agonists targeting the trace amine-associated receptor 1.Science advances · 2024Article
- Antibiotic class with potent in vivo activity targeting lipopolysaccharide synthesis in Gram-negative bacteria.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- Benzothiazole DNA gyrase inhibitors and their conjugates with siderophore mimics: design, synthesis and evaluation.RSC advances · 2024Article
- Discovery and druggability evaluation of pyrrolamide-type GyrB/ParE inhibitor against drug-resistant bacterial infection.Acta pharmaceutica Sinica. B · 2023Article
- Exploring the 5-Substituted 2-Aminobenzothiazole-Based DNA Gyrase B Inhibitors Active against ESKAPE Pathogens.ACS omega · 2023Article
- New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-IntermediateJournal of medicinal chemistry · 2023Article
- Developments in Non-Intercalating Bacterial Topoisomerase Inhibitors: Allosteric and ATPase Inhibitors of DNA Gyrase and Topoisomerase IV.Pharmaceuticals (Basel, Switzerland) · 2023Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
38 authors at 7 institutions in 5 countries.
Andrej Emanuel CotmanFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID 0000-0003-2528-396X
Martina DurcikFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID 0000-0002-9218-1771
Davide Benedetto TizFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.
Federica FulgheriFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID 0000-0002-7858-1605
Daniela SecciFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.
Maša SterleFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID 0000-0003-3898-5194
Štefan MožinaFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID 0000-0002-7416-6981
Žiga SkokFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.
Nace ZidarFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID 0000-0003-1905-0158
Anamarija ZegaFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID 0000-0003-4065-0019
Janez IlašFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID 0000-0002-0124-0474
Lucija Peterlin MašičFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.
Tihomir TomašičFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID 0000-0001-5534-209X
Diarmaid HughesDepartment of Medical Biochemistry and Microbiology, Uppsala University, Husargatan 3, 75123 Uppsala, Sweden.
Douglas L HusebyDepartment of Medical Biochemistry and Microbiology, Uppsala University, Husargatan 3, 75123 Uppsala, Sweden.ORCID 0000-0001-9974-578X
Sha CaoDepartment of Medical Biochemistry and Microbiology, Uppsala University, Husargatan 3, 75123 Uppsala, Sweden.
Linnéa GaroffDepartment of Medical Biochemistry and Microbiology, Uppsala University, Husargatan 3, 75123 Uppsala, Sweden.
Talía Berruga FernándezDepartment of Medical Biochemistry and Microbiology, Uppsala University, Husargatan 3, 75123 Uppsala, Sweden.ORCID 0000-0001-6459-1397
Paraskevi GiachouDepartment of Medical Biochemistry and Microbiology, Uppsala University, Husargatan 3, 75123 Uppsala, Sweden.
Lisa CroneDepartment of Medical Biochemistry and Microbiology, Uppsala University, Husargatan 3, 75123 Uppsala, Sweden.
Ivailo SimoffDrug Optimization and Pharmaceutical Profiling Platform (UDOPP), Department of Pharmacy, Uppsala University, Husargatan 3, 75123 Uppsala, Sweden.ORCID 0000-0001-6522-7191
Richard SvenssonDrug Optimization and Pharmaceutical Profiling Platform (UDOPP), Department of Pharmacy, Uppsala University, Husargatan 3, 75123 Uppsala, Sweden.
Bryndis BirnirDepartment of Medical Cell Biology, Uppsala University, Husargatan 3, 75123 Uppsala, Sweden.
Sergiy V KorolDepartment of Medical Cell Biology, Uppsala University, Husargatan 3, 75123 Uppsala, Sweden.ORCID 0000-0001-8279-2790
Zhe JinDepartment of Medical Cell Biology, Uppsala University, Husargatan 3, 75123 Uppsala, Sweden.
Francisca VicenteFundación MEDINA, Avenida del Conocimiento 34, Parque Tecnológico Ciencias de la Salud, 18016 Granada, Spain.
Maria C RamosFundación MEDINA, Avenida del Conocimiento 34, Parque Tecnológico Ciencias de la Salud, 18016 Granada, Spain.ORCID 0000-0002-3674-615X
Mercedes de la CruzFundación MEDINA, Avenida del Conocimiento 34, Parque Tecnológico Ciencias de la Salud, 18016 Granada, Spain.
Björn GlinghammarDepartment Chemical Process and Pharmaceutical Development, Unit Chemical and Pharmaceutical Safety, RISE Research Institutes of Sweden, 15136 Södertälje, Sweden.
Lena LenhammarDepartment of Medical Sciences, Uppsala University Hospital, 75185 Uppsala, Sweden.
Sara R HendersonDepartment of Biochemistry and Metabolism, John Innes Centre, Norwich Research Park, Norwich NR4 7UH, U.K.ORCID 0000-0003-2078-639X
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.
Guido V JanssenMedicinal Chemistry Division, Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands.
Geert Jan SterkMedicinal Chemistry Division, Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands.
Danijel KikeljFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.
University of Ljubljana · SIUppsala University · SEJohn Innes Centre · GBFundación Medina · ESVrije Universiteit Amsterdam · NLRISE Research Institutes of Sweden · SEUppsala University Hospital · SE
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
We have developed compounds with a promising activity against
Indexed as
Acinetobacter baumanniiTopoisomerase II InhibitorsAnti-Bacterial AgentsBenzothiazolesDNA GyraseEscherichia coliHumansMicrobial Sensitivity TestsPseudomonas aeruginosaAnti-Bacterial AgentsBenzothiazolesDNA GyraseTopoisomerase II Inhibitors
Identifiers
What OpenQuestion holds
Textmetadata
LicenceCC BY
Read underepoch 390
Registered trials
None linked
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.