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

研究成果: Article査読

31 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)4089-4100
ページ数12
ジャーナルBioorganic and Medicinal Chemistry
12
15
DOI
出版ステータスPublished - 2004 8 1
外部発表はい

ASJC Scopus subject areas

  • 生化学
  • 分子医療
  • 分子生物学
  • 薬科学
  • 創薬
  • 臨床生化学
  • 有機化学

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