Synthesis and biological evaluation of 5-carbamoyl-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors.

Goto, Taiji; Shiina, Akiko; Yoshino, Toshiharu; Mizukami, Kiyoshi; Hirahara, Kazuki; Suzuki, Osamu; Sogawa, Yoshitaka; Takahashi, Tomoko; Mikkaichi, Tsuyoshi; Nakao, Naoki; Takahashi, Mizuki; Hasegawa, Masashi; Sasaki, Shigeki

Goto, Taiji; Shiina, Akiko; Yoshino, Toshiharu; Mizukami, Kiyoshi; Hirahara, Kazuki; Suzuki, Osamu; Sogawa, Yoshitaka; Takahashi, Tomoko; Mikkaichi, Tsuyoshi; Nakao, Naoki; Takahashi, Mizuki; Hasegawa, Masashi; Sasaki, Shigeki.

Affiliation

Goto T; R&D Division, Daiichi Sankyo Co., Ltd, 1-2-58, Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan; Graduate School of Pharmaceutical Sciences, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan. Electronic address: goto.taiji.kt@daiichisankyo.co.jp.

Bioorg Med Chem ; 21(22): 7025-37, 2013 Nov 15.

Article in En | MEDLINE | ID: mdl-24094436

Subject(s)

Cyclic Nucleotide Phosphodiesterases, Type 4/chemistry; Phosphodiesterase 4 Inhibitors/chemical synthesis; Phosphodiesterase 4 Inhibitors/pharmacology; Pyridones/chemical synthesis; Pyridones/pharmacology; Pyrimidines/chemical synthesis; Pyrimidines/pharmacology; Animals; Anti-Inflammatory Agents/chemical synthesis; Anti-Inflammatory Agents/pharmacology; Anti-Inflammatory Agents/therapeutic use; Binding Sites; Catalytic Domain; Cells, Cultured; Crystallography, X-Ray; Cyclic Nucleotide Phosphodiesterases, Type 4/metabolism; Enzyme Activation/drug effects; Humans; Lipopolysaccharides/toxicity; Lung Diseases/chemically induced; Lung Diseases/drug therapy; Mice; Phosphodiesterase 4 Inhibitors/therapeutic use; Pyridones/therapeutic use; Pyrimidines/chemistry; Pyrimidines/therapeutic use; Spleen/cytology; Spleen/drug effects; Spleen/metabolism; Tumor Necrosis Factor-alpha/metabolism

Key words

2-Phenylpyrimidine; COPD; Crystallography; PDE4; PDE4 inhibitor; PDE4B; cAMP

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridones / Pyrimidines / Cyclic Nucleotide Phosphodiesterases, Type 4 / Phosphodiesterase 4 Inhibitors Type of study: Prognostic_studies Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2013 Type: Article

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