Orally active PDE4 inhibitors with therapeutic potential.
Basic Information
ID: ALA1147610
Journal: Bioorg Med Chem Lett
Title: Orally active PDE4 inhibitors with therapeutic potential.
Authors: Ochiai H, Ohtani T, Ishida A, Kishikawa K, Obata T, Nakai H, Toda M.
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.
CiteXplore: 14980691
DOI: 10.1016/j.bmcl.2003.12.018
Patent ID: ┄