New 2-amino-pyridinyl-N-acylhydrazones: Synthesis and identification of their mechanism of anti-inflammatory action
•A new n-acylhydrazone was synthetized and presented anti-inflammatory effect.•LASSBio-1828 inhibited p-38 activity, cell migration and cytokine production.•LASSBio-1828 reduced inflammatory pain response.•Data are suggestive that LASSBio-1828 can be considered as a good anti-inflammatory drug candi...
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Veröffentlicht in: | Biomedicine & pharmacotherapy 2020-03, Vol.123, p.109739-109739, Article 109739 |
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Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | •A new n-acylhydrazone was synthetized and presented anti-inflammatory effect.•LASSBio-1828 inhibited p-38 activity, cell migration and cytokine production.•LASSBio-1828 reduced inflammatory pain response.•Data are suggestive that LASSBio-1828 can be considered as a good anti-inflammatory drug candidate.
The main aim of this paper was the synthesis and the evaluation of the anti-inflammatory activity of LASSBio-1828 (an amino-pyridinyl-N-acylhydrazone) and its respective hydrochloride, based on a p38α MAPK inhibitor (LASSBio-1824) previously synthesized by our group.
The compounds were tested regarding their cell viability effect and on acute models of inflammation such as formalin-induced licking test, cell migration and inflammatory mediators quantification.
Treatment with the compounds inhibited p38α, reduced inflammatory pain, cell migration and inflammatory mediators that participate on the MAPK pathway such as TNF-α and IL-1β.
Taken together, these results suggest that the synthesis of the corresponding hydrochloride of LASSBio-1828 enhanced its potency as a p38 inhibitor, and also that this compound could be considered a good anti-inflammatory drug candidate after further studies. |
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ISSN: | 0753-3322 1950-6007 |
DOI: | 10.1016/j.biopha.2019.109739 |