Author/Authors :
Tatsuzo Ukita، نويسنده , , Masakatsu Sugahara، نويسنده , , Yoshihiro Terakawa، نويسنده , , Tooru Kuroda، نويسنده , , Kazuteru Wada، نويسنده , , Aya Nakata، نويسنده , , Hideo Kikkawa، نويسنده , , Katsuo Ikezawa، نويسنده , , Kazuaki Naito، نويسنده ,
Abstract :
A novel series of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives has been prepared. These compounds showed potent PDE4 inhibitory activities and a broad margin between the Ki value of the rolipram binding affinity and the IC50 value of PDE4 inhibition. They also exhibited potent inhibitory activities toward LPS-induced TNF-α production in mice.