ArticleEuropean journal of medicinal chemistry2017
Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
Article in European journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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Who cites it
20 citing papers in PubMed, 60 citations in OpenAlex.
- Ligand-based discovery of novel N-arylpyrrole derivatives as broad-spectrum antimicrobial agents with antibiofilm and anti-virulence activity.Journal of enzyme inhibition and medicinal chemistry · 2025Article
- 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
- Phenyltriazole-based sulfonamides: novel dual-target agents against MRSA biofilms and resistant pathogens.RSC advances · 2025Article
- Discovery and biological evaluation of nitrofuranyl-pyrazolopyrimidine hybrid conjugates as potent antimicrobial agents targetingRSC medicinal chemistry · 2025Article
- Rational design and synthesis of novel phenyltriazole derivatives targeting MRSA cell wall biosynthesis.RSC advances · 2024Article
- Article
- 4-Trifluoromethyl bithiazoles as broad-spectrum antimicrobial agents for virus-related bacterial infections or co-infections.RSC medicinal chemistry · 2024Article
- Synthesis and structure-activity relationship of novel thiazole aminoguanidines against MRSA andRSC medicinal chemistry · 2024Article
- Novel phenylthiazoles with aRSC advances · 2024Article
- Naphthylthiazoles: a class of broad-spectrum antifungals.RSC medicinal chemistry · 2023Article
- Exploration of NMI-MsCl mediated amide bond formation for the synthesis of novel 3,5-substituted-1,2,4-oxadiazole derivatives: synthesis, evaluation of anti-inflammatory activity and molecular docking studies.Molecular diversity · 2023Article
- Expanding the structure-activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents.RSC medicinal chemistry · 2023Article
- Design, synthesis and molecular docking studies of some 1-(5-(2-fluoro-5-(trifluoromethoxy)phenyl)-1,2,4-oxadiazol-3-yl)piperazine derivatives as potential anti-inflammatory agents.Molecular diversity · 2022Article
- The Anti-MRSA Activity of Phenylthiazoles: A Comprehensive Review.Current pharmaceutical design · 2022Review
- Unravelling the anticancer potency of 1,2,4-triazole-N-arylamide hybrids through inhibition of STAT3: synthesis and in silico mechanistic studies.Molecular diversity · 2021Article
- Identification of a Phenylthiazole Small Molecule with Dual Antifungal and Antibiofilm Activity Against Candida albicans and Candida auris.Scientific reports · 2019Article
- Peptidoglycan pathways: there are still more!RSC advances · 2019Review
- Article
- Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA).European journal of medicinal chemistry · 2018Article
Corrections and comments
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Authors and funding
12 authors at 3 institutions in 2 countries.
Funding
Abstract
The promising antibacterial potency of arylthiazole antibiotics is offset by their limited activity against intracellular bacteria (namely methicillin-resistant Staphylococcus aureus (MRSA)), similar to many clinically-approved antibiotics. The failure to target these hidden pathogens is due to the compounds' lack of proper characteristics to accumulate intracellularly. Fine tuning of the size and polar-surface-area of the linking heteroaromatic ring provided a new series of 5-thiazolylarylthiazoles with balanced properties that allow them to sufficiently cross and accumulate inside macrophages infected with MRSA. The most promising compound 4i exhibited rapid bactericidal activity, good metabolic stability and produced over 80% reduction of intracellular MRSA in infected macrophages.
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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.