ArticleEuropean journal of medicinal chemistry2018
Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA).
Article in European journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 53 citations in OpenAlex.
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- Triazole-functionalized compounds as promising antifungal agents: Synthesis, biological evaluation, and mechanistic insights.Naunyn-Schmiedeberg's archives of pharmacology · 2025Article
- Development of carboximidamide small molecule nanogels as potent antimicrobial functional drug delivery systems.RSC advances · 2025Article
- Hit-to-Lead Optimization of Acetazolamide-Based Bacterial Carbonic Anhydrase Inhibitors with Efficacy In Vivo for Treatment of Vancomycin-Resistant Enterococci Septicemia.Journal of medicinal chemistry · 2025Article
- Phenyltriazole-based sulfonamides: novel dual-target agents against MRSA biofilms and resistant pathogens.RSC advances · 2025Article
- Rational design and synthesis of novel phenyltriazole derivatives targeting MRSA cell wall biosynthesis.RSC advances · 2024Article
- Phenylthiazoles with potent & optimum selectivity towardRSC medicinal chemistry · 2024Article
- Naphthylthiazoles: a class of broad-spectrum antifungals.RSC medicinal chemistry · 2023Article
- Expanding the structure-activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents.RSC medicinal chemistry · 2023Article
- Synthesis and Development ofAntibiotics (Basel, Switzerland) · 2023Article
- A Review of the Biological Activity of Amidrazone Derivatives.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Acetylene containing 2-(2-hydrazinyl)thiazole derivatives: design, synthesis, andRSC advances · 2022Article
- The Anti-MRSA Activity of Phenylthiazoles: A Comprehensive Review.Current pharmaceutical design · 2022Review
- High-throughput screening identifies a novel natural product-inspired scaffold capable of inhibiting Clostridioides difficile in vitro.Scientific reports · 2021Article
- Thiazole Ring-A Biologically Active Scaffold.Molecules (Basel, Switzerland) · 2021Review
- Identification of a Phenylthiazole Small Molecule with Dual Antifungal and Antibiofilm Activity Against Candida albicans and Candida auris.Scientific reports · 2019Article
- An aryl isonitrile compound with an improved physicochemical profile that is effective in two mouse models of multidrug-resistant Staphylococcus aureus infection.Journal of global antimicrobial resistance · 2019Article
- Peptidoglycan pathways: there are still more!RSC advances · 2019Review
- Design, synthesis, and antibacterial evaluation of novel derivatives of NPS-2143 for the treatment of methicillin-resistant S. aureus (MRSA) infection.The Journal of antibiotics · 2019Article
Corrections and comments
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Authors and funding
12 authors at 3 institutions in 2 countries.
Funding
Abstract
The promising activity of phenylthiazoles against multidrug-resistant bacterial pathogens, in particular MRSA, has been hampered by their limited systemic applicability, due to their rapid metabolism by hepatic microsomal enzymes, resulting in short half-lives. Here, we investigated a series of phenylthiazoles with alkynyl side-chains that were synthesized with the objective of improving stability to hepatic metabolism, extending the utility of phenylthiazoles from topical applications to treatment of a more invasive, systemic MRSA infections. The most promising compounds inhibited the growth of clinically-relevant isolates of MRSA in vitro at concentrations as low as 0.5 μg/mL, and exerted their antibacterial effect by interfering with bacterial cell wall synthesis via inhibition of undecaprenyl diphosphate synthase and undecaprenyl diphosphate phosphatase. We also identified two phenylthiazoles that successfully eradicated MRSA inside infected macrophages. In vivo PK analysis of compound 9 revealed promising stability to hepatic metabolism with a biological half-life of ∼4.5 h. In mice, compound 9 demonstrated comparable potency to vancomycin, and at a lower dose (20 mg/kg versus 50 mg/kg), in reducing the burden of MRSA in a systemic, deep-tissue infection, using the neutropenic mouse thigh-infection model. Compound 9 thus represents a new phenylthiazole lead for the treatment of MRSA infections that warrants further development.
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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.