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May 24, 2026Pharmaceuticals0 citationsOpen Access

Evaluation of Pyrazino[2,1-b]quinazoline-3,6-dione Derivatives for Inflammation

Anti-Inflammatory Evaluation of Pyrazino2,1-bquinazoline-3,6-dione Derivatives Inspired by Fiscalin B

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Authors

MMMárcia S. MartinsMPMadalena PintoIAIsabel F. Almeida

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Overview

Randomized trial evaluates anti-inflammatory effects in skin diseases, suggesting promising therapeutic options.

Key Points

  • This study aims to identify fiscalin B derivatives as high-affinity ligands for NK1R and evaluate their anti-inflammatory effects.
  • Screened a library of fiscalin B derivatives using molecular docking against NK1R.
  • Conducted in vitro assays in HaCaT keratinocytes, RAW264.7 macrophages, and NIH/3T3 fibroblasts.
  • Assessed cytotoxicity, nitric oxide production, and inflammatory protein expression.
  • Several derivatives showed binding affinities comparable to the NK1R antagonist aprepitant.
  • Compounds 2, 3, and 4 reduced lipopolysaccharide-induced nitric oxide production by 41–51%, without significant cytotoxicity.
  • Most compounds demonstrated positive safety profiles despite potential aquatic toxicity.

Cite This Study

Martins et al. (2026) studied this question.

synapsesocial.com/papers/6a12964948a0ea166567300fhttps://doi.org/10.3390/ph19050775
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