Synthesis and Biological Studies of A Novel Series of Catechol Ether Type Derivatives as Potential Phosphodiesterase(PDE) IV Inhibitors

  • Lee, Jae-Mok (Department of Medicinal Chemistry, Cheil Jedang Corp.) ;
  • Lee, Koun-Ho (Department of Medicinal Chemistry, Cheil Jedang Corp) ;
  • Kim, Jong-Hoon (Department of Medicinal Chemistry, Cheil Jedang Corp) ;
  • Song, Seog-Beom (Department of Medicinal Chemistry, Cheil Jedang Corp) ;
  • Chun, Hyung-Ok (Department of Medicinal Chemistry, Cheil Jedang Corp) ;
  • Yeon, Kyu-Jeong (Department of Medicinal Chemistry, Cheil Jedang Corp) ;
  • Kwon, Soon-Ji (Department of Medicinal Chemistry, Cheil Jedang Corp.)
  • Published : 2002.10.01

Abstract

We synthesized various catechol ether type derivatives substituted by the hydrazine moiety and evaluated for their ability to inhibit PDE Ⅳ (Phosphodiesterase Ⅳ). These new compounds were synthesized from 4-methoxy-3-hydroxy benzaldehyde through 5 or 7 steps. Some of them have similar or more potent inhibitory activity against PDE Ⅳ than known PDE Ⅳ inhibitor. Ariflo (SB 207499). Structure activity relationship (SAR) and biological studies of described compounds will be discussed in detail. (omitted)

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