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  • Title: Orally active PDE4 inhibitors with therapeutic potential.
    Author: Ochiai H, Ohtani T, Ishida A, Kishikawa K, Obata T, Nakai H, Toda M.
    Journal: Bioorg Med Chem Lett; 2004 Mar 08; 14(5):1323-7. PubMed ID: 14980691.
    Abstract:
    Based on the successful results in the clinical trial of Ariflo, further optimization of the spatial arrangement of the three pharmacophores (carboxylic acid moiety, nitrile moiety and 3-cyclopentyl-4-methoxyphenyl moiety) in the structure of Ariflo 1 was attempted using a bicyclo[3.3.0]octane template instead of a cyclohexane template. As a result, 2a, 7a and 7b were found to be orally active and were predicted to have an improved therapeutic potential based on evaluation by cross-species and same-species comparisons. Structure-activity relationships (SARs) of these compounds are also discussed.
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