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Bioorg Med Chem Lett. 2003 Jul 21;13(14):2347-50.

Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors.

Author information

1
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.

PMID:
12824031
DOI:
10.1016/s0960-894x(03)00438-4
[Indexed for MEDLINE]

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