Highly potent PDE4 inhibitors with therapeutic potential

…, K Kishikawa, S Yamamoto, H Takeda, T Obata…

文献索引：Ochiai, Hiroshi; Ohtani, Tazumi; Ishida, Akiharu; Kusumi, Kensuke; Kato, Masashi; Kohno, Hiroshi; Odagaki, Yoshihiko; Kishikawa, Katuya; Yamamoto, Susumu; Takeda, Hiroshi; Obata, Takaaki; Nakai, Hisao; Toda, Masaaki Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 17 p. 4645 - 4665

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被引用次数: 20

摘要

The hypothesis that the dose-limiting side effects of PDE4 inhibitors could be mediated via the central nervous system prompted us to design and synthesize a hydrophilic piperidine analog to improve the side effect profile of Ariflo™ 1, which is an orally active second- generation PDE4 inhibitor. During evaluation of various water-soluble piperidine analogs, 2a–b, 11b–14b, and 17a showed therapeutic potential in cross-species comparison ...