ArticleArchiv der Pharmazie2025
NorA Efflux Pump Inhibitors: Expanding SAR Knowledge of Pyrazolo[4,3-c][1,2]benzothiazine 5,5-Dioxide Derivatives.
Article in Archiv der Pharmazie, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
What it found
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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
2 citing papers in PubMed.
- 1,2-Benzothiazine Derivatives as Anti-HIV and Anti-HCV Agents: Structure-Activity Relationships and Research Perspectives.International journal of molecular sciences · 2026Review
- Screening ofFrontiers in microbiology · 2026Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
15 authors.
Funding
Abstract
Antimicrobial resistance (AMR) represents a significant global concern, driven by the overuse of antibiotics. One of the principal mechanisms contributing to AMR is the activity of microbial efflux pumps (EPs), which expel diverse antibiotics out of bacterial cells, thereby rendering them ineffective. Our research aimed to expand the range of molecular classes that inhibit the Staphylococcus aureus EP NorA. In this study, starting from the hit compound pyrazolo[4,3-c][1,2]benzothiazine 5,5-dioxide 1, previously reported as a NorA efflux pump inhibitor (EPI), we undertook medicinal chemistry efforts, which involved the iterative combination of the design and synthesis of new analogues with data obtained through ethidium bromide efflux inhibition assays. Subsequent synergistic assays with ciprofloxacin (CPX) against the resistant strain SA-1199B led to the identification of three potent compounds (3, 10, and 19). The evaluation of these compounds in combination with CPX against NorA-overexpressing and NorA-knockout strains (SA-K2378 and SA-K1902, respectively) confirmed that the observed synergy with CPX is dependent on the presence of NorA. Additionally, the combination of NorA EPIs with CPX reduced biofilm production in NorA-overexpressing strains. These findings enhance our understanding of the structure-activity relationship of pyrazolobenzothiazine derivatives and support the use of EtBr efflux assays for rapid NorA inhibitors' identification.
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Registered trials
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.