ArticleEuropean journal of medicinal chemistry2015
Synthesis and antibacterial evaluation of a novel series of synthetic phenylthiazole compounds against methicillin-resistant Staphylococcus aureus (MRSA).
Article in European journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed.
- Antibiofilm and antibacterial activity of maslinic acid against Vancomycin-Resistant Enterococci (VRE).PloS one · 2026Article
- Phenyltriazole-based sulfonamides: novel dual-target agents against MRSA biofilms and resistant pathogens.RSC advances · 2025Article
- Synthesis and structure-activity relationship of novel thiazole aminoguanidines against MRSA andRSC medicinal chemistry · 2024Article
- Naphthylthiazoles: a class of broad-spectrum antifungals.RSC medicinal chemistry · 2023Article
- Exploring novel aryl/heteroaryl-isosteres of phenylthiazole against multidrug-resistant bacteria.RSC advances · 2023Article
- Article
- Discovery of a novel natural product inhibitor of Clostridioides difficile with potent activity in vitro and in vivo.PloS one · 2022Article
- 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
- Isopropoxy Benzene Guanidine KillsFrontiers in microbiology · 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
- Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.European journal of medicinal chemistry · 2018Article
- Discovery and Development of 8-Substituted Cycloberberine Derivatives as Novel Antibacterial Agents against MRSA.ACS medicinal chemistry letters · 2018Article
- Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA).European journal of medicinal chemistry · 2018Article
- Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.European journal of medicinal chemistry · 2017Article
- Synthesis and biological evaluation of indole core-based derivatives with potent antibacterial activity against resistant bacterial pathogens.The Journal of antibiotics · 2017Article
- Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.Journal of medicinal chemistry · 2017Article
- Bacteriological profiling of diphenylureas as a novel class of antibiotics against methicillin-resistant Staphylococcus aureus.PloS one · 2017Article
- Targeting Multidrug-resistant Staphylococci with an anti-rpoA Peptide Nucleic Acid Conjugated to the HIV-1 TAT Cell Penetrating Peptide.Molecular therapy. Nucleic acids · 2016Article
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
Methicillin-resistant Staphylococcus aureus infections are a significant global health challenge in part due to the emergence of strains exhibiting resistance to nearly all classes of antibiotics. This underscores the urgent need for the rapid development of novel antimicrobials to circumvent this burgeoning problem. Previously, whole-cell screening of a library of 2,5-disubstituted thiazole compounds revealed a lead compound exhibiting potent antimicrobial activity against MRSA. The present study, conducting a more rigorous analysis of the structure-activity relationship of this compound, reveals a nonpolar, hydrophobic functional group is favored at thiazole-C2 and an ethylidenehydrazine-1-carboximidamide moiety is necessary at C5 for the compound to possess activity against MRSA. Furthermore, the MTS assay confirmed analogs 5, 22d, and 25 exhibited an improved toxicity profile (not toxic up to 40 μg/mL to mammalian cells) over the lead 1. Analysis with human liver microsomes revealed compound 5 was more metabolically stable compared to the lead compound (greater than eight-fold improvement in the half-life in human liver microsomes). Collectively the results presented demonstrate the novel thiazole derivatives synthesized warrant further exploration for potential use as future antimicrobial agents for the treatment of multidrug-resistant S. aureus infections.
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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.