Synapse
⌘+K
Synapse
PulseExploreJournal ClubResearchersJournals
Instagram
HomeJournal ClubExplore
April 15, 2026Open Access

Novel Pyrazole-3-Cyano-2-Pyridinone Hybrids as Multitarget Anti-Inflammatory Agents: Synthesis, Computational Modeling, and Biological Evaluation

View Full Paper
Ask AI
Bookmark
Share

Authors

BHBahgat R. M. HusseinISIbrahim M. SalemHAHossameldin A. Aziz

Discussion

Loading...

Member takes

Overview

Novel compounds inhibit inflammatory mediators in macrophages, suggesting potential for improved therapies.

Key Points

  • This research aims to develop and evaluate pyrazole/3-cyano-2-pyridinone hybrids as multi-target anti-inflammatory agents.
  • Synthesis of pyrazole/3-cyano-2-pyridinone hybrids.
  • Evaluation of anti-inflammatory activity in LPS-stimulated RAW 264.7 macrophages.
  • Inhibition assays for NO, iNOS, COX-1, COX-2, LOX, PGE2, and TNF-α.
  • Molecular docking and molecular dynamics simulations for binding analysis.
  • In silico ADME profiling for pharmacokinetic predictions.
  • Compounds 5f, 5g, 5k, and 5m significantly inhibited NO production and iNOS activity.
  • Compound 5m exhibited the strongest effect with IC$_{50}$ of 203.9 μM.
  • Compound 5k showed the highest COX-2 potency with an IC$_{50}$ of 0.92 μM.
  • Compound 5g effectively suppressed PGE2 production with IC$_{50}$ of 152.7 pg/mL.
  • All compounds demonstrated low cytotoxicity (IC$_{50}$ > 85 μM).

Cite This Study

Hussein et al. (2026) studied this question.

synapsesocial.com/papers/69df2c50e4eeef8a2a6b1646https://doi.org/10.5445/ir/1000192140
View Full Paper
Ask AI
Bookmark
Share