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Biomed Pharmacother ; 123: 109739, 2020 Mar.
Article En | MEDLINE | ID: mdl-31918210

AIMS: 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. MAIN METHODS: 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. KEY FINDINGS: 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-1ß. SIGNIFICANCE: 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.


Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/chemical synthesis , Anti-Inflammatory Agents/pharmacology , Benzylidene Compounds/chemistry , Benzylidene Compounds/chemical synthesis , Benzylidene Compounds/pharmacology , Animals , Anti-Inflammatory Agents/administration & dosage , Benzylidene Compounds/administration & dosage , Carrageenan/administration & dosage , Cell Movement/drug effects , Cytokines/drug effects , Drug Design , Formaldehyde/administration & dosage , Mice , Molecular Structure , Nitric Oxide/metabolism , RAW 264.7 Cells , p38 Mitogen-Activated Protein Kinases/drug effects
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