Synthesis of 3,3'-(1-piperidino)substituted methylene-bis-isoxazoles preventing stimulus-induced leukocytes activation
| Autor: | E. Nieddu, R. Minafra, Mauro Mazzei, Edon Melloni |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2003 |
| Předmět: |
Stereochemistry
Neutrophile Cell Pharmaceutical Science Mannich base Stimulus (physiology) Chemical synthesis chemistry.chemical_compound Piperidines Drug Discovery medicine Leukocytes Humans Methylene Protein kinase C chemistry.chemical_classification General Medicine Isoxazoles Hydrocarbons In vitro medicine.anatomical_structure Enzyme chemistry Biophysics Cellular model Signal transduction Cell activation Methane |
| Popis: | Some 3,3'-(1-piperidino)substituted methylene-bis-isoxazoles were prepared via Mannich base and tested to verify their antiinflammatory-related activity. Human neutrophils stimulated with either PMA and f-MLP were used as the cellular model. The efficiency of eight differently substituted compounds (2-9) was established on their capacity to reduce the O(2)(-) production by activated human neutrophils. The rising hydrophobicity in the side-chain of methylene-bis-isoxazoles leads to a distinction in the neutrophil response against the two stimuli, favoring the inhibition of the PMA elicited cell activation and leaving inaffected the f-MLP induced cell responses. Compounds 8 and 9 are particularly active and abolish almost completely the neutrophil activation in the presence of PMA stimulus. |
| Databáze: | OpenAIRE |
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