Orally active PDE4 inhibitors with therapeutic potential

Hiroshi Ochiai, Tazumi Ohtani, Akiharu Ishida, Katuya Kishikawa, Takaaki Obata, Hisao Nakai, Masaaki Toda

Research output: Contribution to journalArticlepeer-review

12 Citations (Scopus)


Based on the successful results in the clinical trial of Ariflo™, further optimization of the spatial arrangement of the three pharmacophores (carboxylic acid moiety, nitrile moiety and 3-cyclopentyl-4-methoxyphenyl moiety) in the structure of Ariflo 1 was attempted using a bicyclo[3· 3·0]octane template instead of a cyclohexane template. As a result, 2a, 7a and 7b were found to be orally active and were predicted to have an improved therapeutic potential based on evaluation by cross-species and same-species comparisons. Structure-activity relationships (SARs) of these compounds are also discussed.

Original languageEnglish
Pages (from-to)1323-1327
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number5
Publication statusPublished - 2004 Mar 8
Externally publishedYes


  • Bicyclo[3·3·0]octane
  • Orally active
  • PDE4 inhibitor
  • Three pharmacophores

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


Dive into the research topics of 'Orally active PDE4 inhibitors with therapeutic potential'. Together they form a unique fingerprint.

Cite this