Orally active PDE4 inhibitors with therapeutic potential

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

研究成果: Article査読

12 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)1323-1327
ページ数5
ジャーナルBioorganic and Medicinal Chemistry Letters
14
5
DOI
出版ステータスPublished - 2004 3月 8
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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