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Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors |
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| Authors: | Ukita Tatsuzo Sugahara Masakatsu Terakawa Yoshihiro Kuroda Tooru Wada Kazuteru Nakata Aya Kikkawa Hideo Ikezawa Katsuo Naito Kazuaki |
| Affiliation: | Discovery Research Laboratory, Tanabe Seiyaku Co., Ltd., 3-16-89, Kashima, Yodogawa, 532-8505, Osaka, Japan. t-ukita@tanabe.co.jp |
| 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 K(i) value of the rolipram binding affinity and the IC(50) value of PDE4 inhibition. They also exhibited potent inhibitory activities toward LPS-induced TNF-alpha production in mice. |
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