Design, synthesis, and biological evaluation of new phosphodiesterase type 4 inhibitors

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

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)

Abstract

The mode of interaction with enzyme is hypothesized based on the SAR data. The design, synthesis, and biological evaluation of new phosphodiesterase type 4 inhibitors, which possess new templates instead of a cyclohexane ring, are described. The mode of interaction with the enzyme is discussed based on the structure-activity relationship (SAR) data obtained for the synthesized inhibitors. Furthermore, the roles of three pharmacophores, a catechol moiety, a nitrile moiety, and acidic moieties, are discussed using in silico docking studies. More detailed biological evaluations of selected compounds are also presented.

Original languageEnglish
Pages (from-to)5063-5078
Number of pages16
JournalBioorganic and Medicinal Chemistry
Volume12
Issue number19
DOIs
Publication statusPublished - 2004 Oct 1
Externally publishedYes

ASJC Scopus subject areas

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

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