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

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1297-303. doi: 10.1016/j.bmcl.2008.01.028. Epub 2008 Jan 11.

Abstract

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

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

Substances

  • Isoenzymes
  • Phosphodiesterase 4 Inhibitors
  • Phosphodiesterase Inhibitors
  • Thiadiazines
  • Triazoles