Ukita Tatsuzo, Sugahara Masakatsu, Terakawa Yoshihiro, Kuroda Tooru, Wada Kazuteru, Nakata Aya, Kikkawa Hideo, Ikezawa Katsuo, Naito Kazuaki
Discovery Research Laboratory, Tanabe Seiyaku Co., Ltd., 3-16-89, Kashima, Yodogawa, 532-8505, Osaka, Japan.
Bioorg Med Chem Lett. 2003 Jul 21;13(14):2347-50. doi: 10.1016/s0960-894x(03)00438-4.
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.
已制备了一系列新型的1-吡啶基异喹啉和1-吡啶基二氢异喹啉衍生物。这些化合物显示出强效的磷酸二酯酶4（PDE4）抑制活性，并且咯利普兰结合亲和力的K(i)值与PDE4抑制的IC(50)值之间有很大差距。它们还对小鼠中脂多糖诱导的肿瘤坏死因子-α（TNF-α）产生表现出强效抑制活性。
