Abstract
The latest scientific findings concerning PDE7 and PDE4 inhibition suggest that selective small-molecule inhibitors of both enzymes could provide a novel approach to treat a variety of immunological diseases. In this context, we describe a new series of quinazoline derivatives from quinazolin-4-thiones which include a substituted biphenyl fragment. Some of these compounds show inhibitory potencies at sub-micromolar levels against the catalytic domain of PDE7.
Copyright © 2013 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Cyclic Nucleotide Phosphodiesterases, Type 7 / antagonists & inhibitors*
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Cyclic Nucleotide Phosphodiesterases, Type 7 / chemistry
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Phosphodiesterase Inhibitors / chemical synthesis*
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Phosphodiesterase Inhibitors / chemistry
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Phosphodiesterase Inhibitors / pharmacology*
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Quinazolines / chemical synthesis*
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Quinazolines / chemistry
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Quinazolines / pharmacology*
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Structure-Activity Relationship
Substances
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Phosphodiesterase Inhibitors
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Quinazolines
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Cyclic Nucleotide Phosphodiesterases, Type 7