Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors

Bioorg Med Chem. 2013 Apr 15;21(8):2370-2378. doi: 10.1016/j.bmc.2013.01.067. Epub 2013 Feb 5.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyclic Nucleotide Phosphodiesterases, Type 7 / antagonists & inhibitors*
  • Cyclic Nucleotide Phosphodiesterases, Type 7 / chemistry
  • Phosphodiesterase Inhibitors / chemical synthesis*
  • Phosphodiesterase Inhibitors / chemistry
  • Phosphodiesterase Inhibitors / pharmacology*
  • Quinazolines / chemical synthesis*
  • Quinazolines / chemistry
  • Quinazolines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Phosphodiesterase Inhibitors
  • Quinazolines
  • Cyclic Nucleotide Phosphodiesterases, Type 7