Title of article :
Design, synthesis, and biological evaluation of new phosphodiesterase type 4 inhibitors Original Research Article
Author/Authors :
Hiroshi Ochiai، نويسنده , , Yoshihiko Odagaki، نويسنده , , Tazumi Ohtani، نويسنده , , Akiharu Ishida، نويسنده , , Kensuke Kusumi، نويسنده , , Katuya Kishikawa، نويسنده , , SUSUMU YAMAMOTO، نويسنده , , Hiroshi Takeda، نويسنده , , Takaaki Obata، نويسنده , , Kaoru Kobayashi، نويسنده , , Hisao Nakai، نويسنده , , Masaaki Toda، نويسنده ,
Abstract :
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.