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Synthesis and structure-activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitors
Authors:Gewald Rainer  Rueger Carla  Grunwald Christian  Egerland Ute  Hoefgen Norbert
Affiliation:biocrea GmbH, Meissner Strasse 191, 01445 Radebeul, Germany. rainer.gewald@biocrea.com
Abstract:The synthesis and SAR studies of a series of structurally novel inhibitors of PDE7 are discussed. The best compounds from the series display low nanomolar inhibitory activity and are selective versus other PDE isoenzymes.
Keywords:PDE7 inhibitor   Phosphodiesterase   Dihydronaphthyridinedione   Structure-activity relationship   Molecular docking
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