Identification of the 5, 5-dioxo-7, 8-dihydro-6H-thiopyrano [3, 2-d] pyrimidine derivatives as highly selective PDE4B inhibitors

…, Y Sogawa, K Mizukami, N Takagi, T Yoshitomi…

文献索引：Goto, Taiji; Shiina, Akiko; Murata, Takeshi; Tomii, Masato; Yamazaki, Takanori; Yoshida, Ken-Ichi; Yoshino, Toshiharu; Suzuki, Osamu; Sogawa, Yoshitaka; Mizukami, Kiyoshi; Takagi, Nana; Yoshitomi, Tomomi; Etori, Maki; Tsuchida, Hiroshi; Mikkaichi, Tsuyoshi; Nakao, Naoki; Takahashi, Mizuki; Takahashi, Hisashi; Sasaki, Shigeki Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 3 p. 893 - 899

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被引用次数: 12

摘要

Abstract A PDE4B subtype selective inhibitor is expected to have a wider therapeutic window than non-selective PDE4 inhibitors. In this Letter, two series of 7, 8-dihydro-6H- thiopyrano [3, 2-d] pyrimidine derivatives and 5, 5-dioxo-7, 8-dihydro-6H-thiopyrano [3, 2-d] pyrimidine derivatives were evaluated for their PDE4B subtype selectivity using human PDE4B2 and PDE4D2 full length enzymes. To improve their PDE4B selectivity over ...