Identification of a potent new chemotype for the selective inhibition of PDE4.

Medicinal Chemistry


A series of substituted 3,6-diphenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines were prepared and analyzed as inhibitors of phosphodiesterase 4 (PDE4). Synthesis, structure-activity relationships, and the selectivity of a highly potent analogue against related phosphodiesterase isoforms are presented.


Skoumbourdis, Amanda P; Huang, Ruili; Southall, Noel; Leister, William; Guo, Vicky; Cho, Ming-Hsuang; Inglese, James; Nirenberg, Marshall; Austin, Christopher; Xia, Menghang; Thomas, Craig;


  • Humans
  • Isoenzymes/ antagonists & inhibitors
  • Phosphodiesterase 4 Inhibitors
  • Phosphodiesterase Inhibitors/ chemistry
  • Phosphodiesterase Inhibitors/ pharmacology
  • Structure-Activity Relationship
  • Thiadiazines/ chemistry
  • Thiadiazines/ pharmacology
  • Triazoles/ chemistry
  • Triazoles/ pharmacology

External Links