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Bioorg Med Chem
; 21(8): 2370-2378, 2013 Apr 15.
Article
in English
| MEDLINE
| ID: mdl-23454131
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.
Subject(s)
Cyclic Nucleotide Phosphodiesterases, Type 7/antagonists & inhibitors , Phosphodiesterase Inhibitors/chemical synthesis , Phosphodiesterase Inhibitors/pharmacology , Quinazolines/chemical synthesis , Quinazolines/pharmacology , Cyclic Nucleotide Phosphodiesterases, Type 7/chemistry , Phosphodiesterase Inhibitors/chemistry , Quinazolines/chemistry , Structure-Activity Relationship
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