Abstract
New imidazo[1,2-a]quinoxaline derivatives have been synthesised by condensation of an appropriate alpha-aminoalcohol with a quinoxaline followed by intramolecular cyclisation and nucleophilic substitutions. Their phosphodiesterase inhibitory activities have been assessed on a preparation of the PDE4 isoform purified from a human alveolar epithelial cell line (A549). These studies showed potent inhibitory properties that emphasize the importance of a methyl amino group at position 4 and a weakly hindered group at position 1.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors*
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3',5'-Cyclic-AMP Phosphodiesterases / isolation & purification
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Cell Line
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Cyclic Nucleotide Phosphodiesterases, Type 4
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Drug Design
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Epithelial Cells / enzymology
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Humans
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Inflammation / prevention & control
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Inhibitory Concentration 50
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Lung / cytology
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Quinoxalines / chemical synthesis*
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Quinoxalines / pharmacology*
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Structure-Activity Relationship
Substances
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Quinoxalines
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3',5'-Cyclic-AMP Phosphodiesterases
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Cyclic Nucleotide Phosphodiesterases, Type 4