Discovery of new orally active phosphodiesterase (PDE4) inhibitors

Hiroshi Ochiai, Akiharu Ishida, Tazumi Ohtani, Kensuke Kusumi, Katuya Kishikawa, Susumu Yamamoto, Hiroshi Takeda, Takaaki Obata, Hisao Nakai, Masaaki Toda

Research output: Contribution to journalArticlepeer-review

14 Citations (Scopus)


A series of 4-anilinopyrazolopyridine derivatives were synthesized and biologically evaluated as inhibitors of phosphodiesterase (PDE4). Chemical modification of 3, a structurally new chemical lead that was found in our in-house library, was focused on 1- and 3-substituents. Full details of the discovery of a new orally active chemical lead 5 are presented. Structure-activity relationship data, pharmacological evaluation, and the subtype selectivity study are also presented.

Original languageEnglish
Pages (from-to)1098-1104
Number of pages7
JournalChemical and Pharmaceutical Bulletin
Issue number9
Publication statusPublished - 2004 Sep
Externally publishedYes


  • 4-anilinopyrazolopyridine
  • Orally active
  • Phosphodiesterase (PDE4) inhibitor
  • Subtype selective

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery


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