ArticleMolecules (Basel, Switzerland)2013
Design, synthesis and evaluation of the antibacterial enhancement activities of amino dihydroartemisinin derivatives.
Article in Molecules (Basel, Switzerland), 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 35 citations in OpenAlex.
- Artesunate, EDTA, and colistin work synergistically against MCR-negative and -positive colistin-resistanteLife · 2025Article
- Development of pharmacophore models for AcrB protein and the identification of potential adjuvant candidates for overcoming efflux-mediated colistin resistance.RSC medicinal chemistry · 2024Article
- Research Progress of Natural Products with the Activity of Anti-nonalcoholic Steatohepatitis.Mini reviews in medicinal chemistry · 2024Review
- Dihydroartemisinin ameliorates innate inflammatory response induced byJournal of pharmaceutical analysis · 2023Article
- Enhancing activity of β-lactam and fluoroquinolones antibiotics by artemisinin and its derivatives against MDRFrontiers in veterinary science · 2022Article
- Artemisinin derivative DHA27 enhances the antibacterial effect of aminoglycosides againstFrontiers in pharmacology · 2022Article
- In search of therapeutic candidates for HIV/AIDS: rational approaches, design strategies, structure-activity relationship and mechanistic insights.RSC advances · 2021Review
- Dihydroartemisinin-Loaded Chitosan Nanoparticles Inhibit the Rifampicin-ResistantFrontiers in microbiology · 2021Article
- Dihydroartemisinin Prevents Progression and Metastasis of Head and Neck Squamous Cell Carcinoma by Inhibiting Polarization of Macrophages in Tumor Microenvironment.OncoTargets and therapy · 2020Article
- Nanostructured Dihydroartemisinin Plus Epirubicin Liposomes Enhance Treatment Efficacy of Breast Cancer by Inducing Autophagy and Apoptosis.Nanomaterials (Basel, Switzerland) · 2018Article
- Interaction between autophagy and senescence is required for dihydroartemisinin to alleviate liver fibrosis.Cell death & disease · 2017Article
- Application of the Triazolization Reaction to Afford Dihydroartemisinin Derivatives with Anti-HIV Activity.Molecules (Basel, Switzerland) · 2017Article
- Design of New Antibacterial Enhancers Based on AcrB's Structure and the Evaluation of Their Antibacterial Enhancement Activity.International journal of molecular sciences · 2016Article
- Design, Synthesis and Cytotoxicity of Novel Dihydroartemisinin-Coumarin Hybrids via Click Chemistry.Molecules (Basel, Switzerland) · 2016Article
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Artemisinin (ART) and its derivatives artesunate (AS), dihydroartemisinin (DHA) are a group of drugs containing a sesquiterpene lactone used to treat malaria. Previously, AS was shown to not have antibacterial activity but to significantly increase the antibacterial activities of β-lactam antibiotics against E. coli. Herein, molecular docking experiments showed that ART, AS and DHA could dock into AcrB very well, especially DHA and AS; both DHA and AS had the same docking pose. The affinity between AS and AcrB seemed weaker than that of DHA, while the succinate tail of AS, which was like a "bug", could extend in the binding pocket very well. Imitating the parent nucleus of DHA and the succinate tail of AS, twenty-one DHA derivatives 4a-u were designed and synthesized. Among them, seventeen were new compounds. The synergistic effects against E. coli AG100A/pET28a-AcrB showed among the new structures 4k, 4l, 4m, 4n, and 4r exhibited significant synergism with β-lactam antibiotics although they had no direct antibacterial activities themselves. The bacterial growth assay showed that only 4k in combination with ampicillin or cefuroxime could totally inhibit bacterial growth from 0 to 12 h, demonstrating that 4k had the best antibacterial enhancement effect. In conclusion, our results provided a new idea and several candidate compounds for antibacterial activity enhancers against multidrug resistant E. coli.
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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.