Abstract
A series of quinazolinediones and azaquinazolinediones is described which possess potent inhibitory activity toward the calcium-independent phosphodiesterase enzyme (CaIPDE). In vivo testing showed that this in vitro activity translates to animal models predictive of chronic diseases such as depression and inflammation. These results support the hypothesis that inhibition of CaIPDE may lead to useful activity in such chronic diseases.
MeSH terms
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Animals
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Brain / drug effects
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Brain / metabolism
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Chemical Phenomena
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Chemistry
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Male
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Mice
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Phosphodiesterase Inhibitors / chemical synthesis*
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Phosphodiesterase Inhibitors / metabolism
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Phosphodiesterase Inhibitors / pharmacology
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Pyrrolidinones / metabolism
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Pyrrolidinones / pharmacology
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Quinazolines / chemical synthesis*
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Quinazolines / metabolism
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Quinazolines / pharmacology
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Rats
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Rolipram
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Structure-Activity Relationship
Substances
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Phosphodiesterase Inhibitors
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Pyrrolidinones
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Quinazolines
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Rolipram