DISCOVERY OF MICROMOLAR PDE-IV INHIBITORS THAT EXHIBIT MUCH REDUCED AFFINITY FOR THE [H-3]ROLIPRAM BINDING-SITE - 3-NORSORNYLOXY-4-METHOXYPHENYLMETHYLENE OXINDOLES

The synthesis and the in vitro properties of a novel series of potent and selective phosphodiesterase type IV (PDE IV) inhibitors is describ ed. Despite bearing structural similarity to rolipram, several of thes e compounds have much reduced affinity for the [H-3]rolipram binding s ite.