Purposeful search and characteristic of anti-inflammatory activity of sodium (3-R-2-оxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues

Authors

  • V. V. Yakubovska Vinnytsya National Pirogov memorial Medical University,
  • N. М. Seredinska Instute Pharmacology and Toxicology NAMS Ukraine,
  • О. Yu. Voskoboynik Zaporizhzhia State Medical University,
  • G. І. Stepanyuk Vinnytsya National Pirogov memorial Medical University,
  • S. І. Kovalenko Zaporizhzhia State Medical University,

DOI:

https://doi.org/10.14739/2409-2932.2016.1.62036

Keywords:

sodium (3-R-2-oxo-2Н-[1, 2, 4]triazino[2, 3-c]quinazolin-6-il)carboxylates, halogen-containing analogues, molecular docking, anti-inflammatory activity

Abstract

Aim. The approaches for creating  novel agents with anti-inflammatory activity among sodium (3-R-2-oxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues were described in presented article.

Methods and results. Mentioned methods have been based on combination of «in silico» screening with experimental studies. Affinity of studied compounds to the active center of COX-1 and COX-2 enzymes has been shown. Conducted visualization of compound – active site complex allowed to suppose the presence of anti-inflammatory activity of studied compounds.

Conclusions. It was established, that sodium (3-R-2-oxo-2Н-[1,2,4]triazino[2,3-c]quinazoline-6-yl)alkylcarboxylates and their halogen-containing analogues reveal anti-inflammatory activity, the most active was compound DSK-38 (ED50 – 4 mg/kg as against 8 mg/kg of diclofenac sodium). «Structure–activity» relationships features among studied compounds have been discussed.

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How to Cite

1.
Yakubovska VV, Seredinska NМ, Voskoboynik ОY, Stepanyuk GІ, Kovalenko SІ. Purposeful search and characteristic of anti-inflammatory activity of sodium (3-R-2-оxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)alkylcarboxylates and their halogen containing analogues. Current issues in pharmacy and medicine: science and practice [Internet]. 2016Mar.9 [cited 2024Dec.25];(1). Available from: http://pharmed.zsmu.edu.ua/article/view/62036

Issue

No. 1 (2016)

Section

Experimental and clinical pharmacology

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