ArticleAntibiotics (Basel, Switzerland)2023
Antibiofilm and Anti-Quorum-Sensing Activities of Novel Pyrazole and Pyrazolo[1,5-
Article in Antibiotics (Basel, Switzerland), 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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17 citing papers in PubMed, 53 citations in OpenAlex.
- Recent advances in adamantane-linked heterocycles: synthesis and biological activity.Molecular diversity · 2026Review
- Quorum-Sensing Inhibitors as Potential Antibacterial Agents Against Staphylococcus aureus: A Comprehensive Review.Chemistry & biodiversity · 2026Review
- Next-generation anti-infective drugs in the post-antibiotic era: focusing on anti-virulence agents targeting the bacterial quorum sensing system.Frontiers in cellular and infection microbiology · 2026Review
- Synthesis, Characterization, Antimicrobial and Anticancer Evaluation of Novel Heterocyclic Diazene Compounds Derived from 8-Quinolinol.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Exploring novel of 1,2,4-triazolo[4,3-a]quinoxaline sulfonamide regioisomers as anti-diabetic and anti-Alzheimer agents with in-silico molecular docking simulation.Scientific reports · 2025Article
- Antimicrobial activity, synthesis, and docking study of some novel arylazo-1,3-thiazolopyrimidine and arylazo-1,3-thiazolopyridopyrimidine derivatives.BMC chemistry · 2025Article
- Recent advances in the synthesis, reaction, and bio-evaluation potential of purines as precursor pharmacophores in chemical reactions: a review.RSC advances · 2025Review
- Bioactive Fused Pyrazoles Inspired by the Adaptability of 5-Aminopyrazole Derivatives: Recent Review.Molecules (Basel, Switzerland) · 2025Review
- Advances in the Synthesis and SAR of Pyrido[2,3-Current pharmaceutical design · 2025Review
- Innovation of 6-sulfonamide-2RSC advances · 2024Article
- Evaluation of novel compounds as anti-bacterial or anti-virulence agents.Frontiers in cellular and infection microbiology · 2024Review
- One-pot synthesis of pyrazolo[4,3-RSC advances · 2023Article
- Design, green synthesis, and quorum sensing quenching potential of novel 2-oxo-pyridines containing a thiophene/furan scaffold and targeting aRSC advances · 2023Article
- A new class of anti-proliferative activity and apoptotic inducer with molecular docking studies for a novel of 1,3-dithiolo[4,5-RSC advances · 2023Article
- Evaluation of the anti-proliferative activity of 2-oxo-pyridine and 1'RSC advances · 2023Article
- Design and Synthesis of Novel Antimicrobial Agents.Antibiotics (Basel, Switzerland) · 2023Review
- Unveiling the antitumor potential of novel N-(substituted-phenyl)-8-methoxycoumarin-3-carboxamides as dual inhibitors of VEGFR2 kinase and cytochrome P450 for targeted treatment of hepatocellular carcinoma.Frontiers in chemistry · 2023Article
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Nowadays, searching for new anti-infective agents with diverse mechanisms of action has become necessary. In this study, 16 pyrazole and pyrazolo[1,5-a]pyrimidine derivatives were synthesized and assessed for their preliminary antibacterial and antibiofilm activities. All these derivatives were initially screened for their antibacterial activity against six clinically isolated multidrug resistance by agar well-diffusion and broth microdilution methods. The initial screening presented significant antibacterial activity with a bactericidal effect for five compounds, namely 3a, 5a, 6, 9a, and 10a, compared with Erythromycin and Amikacin. These five derivatives were further evaluated for their antibiofilm activity against both S. aureus and P. aeruginosa, which showed strong biofilm-forming activity at their MICs by >60%. The SEM analysis confirmed the biofilm disruption in the presence of these derivatives. Furthermore, anti-QS activity was observed for the five hybrids at their sub-MICs, as indicated by the visible halo zone. In addition, the presence of the most active derivatives reduces the violacein production by CV026, confirming that these compounds yielded anti-QS activity. Furthermore, these compounds showed strong inhibitory action against human carbonic anhydrase (hCA-I and hCA-II) isoforms with IC50 values ranging between 92.34 and 168.84 nM and between 73.2 and 161.22 nM, respectively. Finally, radiosterilization, ADMET, and a docking simulation were performed.
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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.