ArticleEuropean journal of medicinal chemistry2021
4-4-(Anilinomethyl)-3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-ylbenzoic acid derivatives as potent anti-gram-positive bacterial agents.
Article in European journal of medicinal chemistry, 2021. 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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Who cites it
16 citing papers in PubMed, 25 citations in OpenAlex.
- Pyrazole-Derived Antibacterial Compounds Effectively Treat Methicillin-Resistant Staphylococcus Aureus Infections by Inhibiting Aspartate Transcarbamoylase.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Employing diclofenac sodium as a novel therapeutic frontier for Staphylococcus epidermidis infections.Scientific reports · 2025Article
- Antimicrobial Efficacy of Trifluoro-Anilines AgainstInternational journal of molecular sciences · 2025Article
- Insights into SARS-CoV-2: Small-Molecule Hybrids for COVID-19 Treatment.Molecules (Basel, Switzerland) · 2024Review
- Efficient Synthesis of Thiazole-Fused Bisnoralcohol Derivatives as Potential Therapeutic Agents.ACS omega · 2024Article
- Design and Synthesis of 1,3-Diarylpyrazoles and Investigation of Their Cytotoxicity and Antiparasitic Profile.International journal of molecular sciences · 2024Article
- Pyrazole: an emerging privileged scaffold in drug discovery.Future medicinal chemistry · 2023Review
- Development and Antibacterial Properties of 4-[4-(Anilinomethyl)-3-phenylpyrazol-1-yl]benzoic Acid Derivatives as Fatty Acid Biosynthesis Inhibitors.Journal of medicinal chemistry · 2023Article
- C-Type Natriuretic Peptide Acts as a Microorganism-Activated Regulator of the Skin CommensalsBiology · 2023Article
- In Vitro Antimelanoma Properties ofMolecules (Basel, Switzerland) · 2022Article
- Development of 4-[4-(Anilinomethyl)-3-phenyl-pyrazol-1-yl] Benzoic Acid Derivatives as Potent Anti-Staphylococci and Anti-Enterococci Agents.Antibiotics (Basel, Switzerland) · 2022Article
- A Review of the Recent Development in the Synthesis and Biological Evaluations of Pyrazole Derivatives.Biomedicines · 2022Review
- Antibacterial pyrazoles: tackling resistant bacteria.Future medicinal chemistry · 2022Review
- Novel pyrazoles as potent growth inhibitors of staphylococci, enterococci andFuture medicinal chemistry · 2022Article
- Repurposing the Sphingosine-1-Phosphate Receptor Modulator Etrasimod as an Antibacterial Agent Against Gram-Positive Bacteria.Frontiers in microbiology · 2022Article
- Synthesis of 3,5-Bis(trifluoromethyl)phenyl-Substituted Pyrazole Derivatives as Potent Growth Inhibitors of Drug-Resistant Bacteria.Molecules (Basel, Switzerland) · 2021Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
A collection of potent antimicrobials consisting of novel 1,3-bis-benzoic acid and trifluoromethyl phenyl derived pyrazoles has been synthesized and tested for antibacterial activity. The majority of trifluoromethyl phenyl derivatives are highly potent growth inhibitors of Gram-positive bacteria and showed low toxicity to human cultured cells. In particular, two compounds (59 and 74) were selected for additional studies. These compounds are highly effective against Staphylococcus aureus as shown by a low minimum inhibitory concentration (MIC), a bactericidal effect in time-kill assays, moderate inhibition of biofilm formation as well as biofilm destruction, and a bactericidal effect against stationary phase cells representing non-growing persister cells. Multistep resistance assays showed a very low tendency for S. aureus and Enterococcus faecalis to develop resistance through mutation. Additionally, in vivo mouse model studies showed no harmful effects at doses up to 50 mg/kg using 14 blood plasma organ toxicity markers or TUNEL assay in liver and kidney. Investigations into the mode of action by performing macromolecular synthesis inhibition studies showed a broad range of inhibitory effects, suggesting targets that have a global effect on bacterial cell function.
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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.