New orally active PDE4 inhibitors with therapeutic potential

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

31 Citations (Scopus)

Abstract

The design, synthesis, and biological evaluation of a series of pyrazolopyridines was carried out. Structural optimization of the aniline moiety of 4-anilinopyrazolopyridine derivative 3a, which is one of the newly discovered chemical leads for PDE4 inhibitors from our in-house library, was performed successfully. The details of the discovery of new orally active PDE4 inhibitors, which are expected to show therapeutic potential, are presented and their structure-activity relationships are discussed. Pharmacological evaluation and pharmacokinetic data for representative compounds are also presented.

Original languageEnglish
Pages (from-to)4089-4100
Number of pages12
JournalBioorganic and Medicinal Chemistry
Volume12
Issue number15
DOIs
Publication statusPublished - 2004 Aug 1
Externally publishedYes

Keywords

  • 4-Anilinopyrazolopyridine
  • Orally active
  • PDE4 inhibitor

ASJC Scopus subject areas

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

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