Design, synthesis and molecular docking of new pyrazole-thiazolidinones as potent anti-inflammatory and analgesic agents with TNF-α inhibitory activity.

Clicks: 838
ID: 265398
2021
Article Quality & Performance Metrics
Overall Quality Improving Quality
83.3 /100
Combines engagement data with AI-assessed academic quality
AI Quality Assessment 🥈 High Quality
82.8 /100
Academic Rigor 88.0%
Novelty 78.0%
Clarity 85.0%
Key Strengths
  • Well-defined research question
  • Strong synthesis and characterization of new compounds
  • In-vivo anti-inflammatory and analgesic evaluation
Areas for Improvement
  • The abstract does not mention the specific animal model used.
  • The abstract does not mention the number of animals used in each group.
  • The abstract does not mention the statistical methods used to analyze the data.
AI Recommendations

Consider providing more details about the statistical analysis performed and the specific animal model used in the in-vivo studies. Expanding on the limitations of the study would also be beneficial.

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Real-world Applications
75%
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Abstract
A new set of derivatives bearing pyrazole-methylenehydrazono-thiazolidinone scaffold 4-23 was designed, synthesized and confirmed by different spectroscopic means and elemental analyses. In-vivo anti-inflammatory and ulcerogenic evaluation was performed for all the newly synthesized derivatives using indomethacin, celecoxib and diclofenac as standard drugs. The compounds 5, 10, 15, 17, 21, 22 appeared to be the most promising candidates producing rapid onset and long duration of anti-inflammatory activity as well as promising GIT safety profile. Furthermore, analgesic evaluation revealed that the compounds 5, 10, 15 and 22 produced potent and long acting analgesia accompanied with significant inhibition of the inflammatory cytokine TNF-α level in comparison with the standard drugs. Molecular docking study of the latter derivatives was also carried out to rationalize their binding affinities and their modes of interactions with the active site of TNF-α.
Reference Key
abd-elkarim2021designbioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Abd El-Karim, Somaia S;Mohamed, Hanaa S;Abdelhameed, Mohamed F;El-Galil E Amr, Abd;Almehizia, Abdulrahman A;Nossier, Eman S;
Journal Bioorganic chemistry
Year 2021
DOI
S0045-2068(21)00204-2
URL
Keywords
molecular docking TNF-α pyrazole anti-inflammatory analgesic thiazolidin-4-one

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