Synthesis and biological evaluation of novel phthalazinone derivatives as topically active phosphodiesterase 4 inhibitors

…, N Inoue, A Hashino, K Kageyama, J Shikaura…

文献索引：Kagayama, Kohei; Morimoto, Tatsuya; Nagata, Seigo; Katoh, Fumitaka; Zhang, Xin; Inoue, Naoki; Hashino, Asami; Kageyama, Kiyoto; Shikaura, Jiro; Niwa, Tomoko Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 19 p. 6959 - 6970

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被引用次数: 22

摘要

Inhibitors of phosphodiesterase 4 (PDE4) are an important class of anti-inflammatory drug that act by inhibiting the production of proinflammatory cytokines, including tumor necrosis factor-α (TNF-α). We have synthesized and evaluated a series of 2-substituted phthalazinone derivatives as PDE4 inhibitors. Structure–activity relationship studies led to the identification of benzylamine-substituted phthalazinones as potent PDE4 inhibitors ...