Synthesis and structure-activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitors

Rainer Gewald; Carla Rueger; Christian Grunwald; Ute Egerland; Norbert Hoefgen

doi:10.1016/j.bmcl.2011.09.065

Synthesis and structure-activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitors

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6652-6. doi: 10.1016/j.bmcl.2011.09.065. Epub 2011 Sep 21.

Authors

Rainer Gewald¹, Carla Rueger, Christian Grunwald, Ute Egerland, Norbert Hoefgen

Affiliation

¹ biocrea GmbH, Meissner Strasse 191, 01445 Radebeul, Germany. rainer.gewald@biocrea.com

PMID: 21983442
DOI: 10.1016/j.bmcl.2011.09.065

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Cyclic Nucleotide Phosphodiesterases, Type 7 / antagonists & inhibitors*
Cyclic Nucleotide Phosphodiesterases, Type 7 / metabolism*
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology*
Humans
Models, Molecular
Naphthyridines / chemistry*
Naphthyridines / pharmacology*
Protein Binding
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Naphthyridines
Cyclic Nucleotide Phosphodiesterases, Type 7
PDE7A protein, human