ArticleJournal of medicinal chemistry2014
Repurposing the antihistamine terfenadine for antimicrobial activity against Staphylococcus aureus.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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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.
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Who cites it
16 citing papers in PubMed, 51 citations in OpenAlex.
- Repurposing rupatadine as topical treatment against methicillin-resistant Staphylococcus aureus.AMB Express · 2025Article
- Artificial photosynthesis directed toward organic synthesis.Nature communications · 2025Article
- Drug Repurposing: Insights into Current Advances and Future Applications.Current medicinal chemistry · 2025Review
- Current Strategies for Combating Biofilm-Forming Pathogens in Clinical Healthcare-Associated Infections.Indian journal of microbiology · 2024Review
- Article
- A Water-Stable Boronate Ester Cage.Journal of the American Chemical Society · 2024Article
- Copper-Catalyzed Regio- and Enantioselective Hydroboration of Difluoroalkyl-Substituted Internal Alkenes.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2023Article
- Drug Repositioning as a Therapeutic Strategy againstInternational journal of molecular sciences · 2023Article
- Bacterial Nosocomial Infections: Multidrug Resistance as a Trigger for the Development of Novel Antimicrobials.Antibiotics (Basel, Switzerland) · 2021Review
- Evaluation of Human Liver Microtissues for Drug Screening onACS infectious diseases · 2021Article
- Brief Overview of Approaches and Challenges in New Antibiotic Development: A Focus On Drug Repurposing.Frontiers in cellular and infection microbiology · 2021Review
- Tree-Based QSAR Model for Drug Repurposing in the Discovery of New Antibacterial Compounds AgainstPharmaceuticals (Basel, Switzerland) · 2020Article
- Antimicrobial Properties on Non-Antibiotic Drugs in the Era of Increased Bacterial Resistance.Antibiotics (Basel, Switzerland) · 2020Review
- Drug Repurposing for the Treatment of Bacterial and Fungal Infections.Frontiers in microbiology · 2019Review
- In Vitro Screening of an FDA-Approved Library Against ESKAPE Pathogens.Current pharmaceutical design · 2017Article
- Drug repurposing as an alternative for the treatment of recalcitrant bacterial infections.Frontiers in microbiology · 2015Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
Staphylococcus aureus is a rapidly growing health threat in the U.S., with resistance to several commonly prescribed treatments. A high-throughput screen identified the antihistamine terfenadine to possess, previously unreported, antimicrobial activity against S. aureus and other Gram-positive bacteria. In an effort to repurpose this drug, structure-activity relationship studies yielded 84 terfenadine-based analogues with several modifications providing increased activity versus S. aureus and other bacterial pathogens, including Mycobacterium tuberculosis. Mechanism of action studies revealed these compounds to exert their antibacterial effects, at least in part, through inhibition of the bacterial type II topoisomerases. This scaffold suffers from hERG liabilities which were not remedied through this round of optimization; however, given the overall improvement in activity of the set, terfenadine-based analogues provide a novel structural class of antimicrobial compounds with potential for further characterization as part of the continuing process to meet the current need for new antibiotics.
Indexed as
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What OpenQuestion holds
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.