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ID: ALA1221357
Journal: Bioorg Med Chem Lett
Title: The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors.
Authors: Aspiotis R, Deschênes D, Dubé D, Girard Y, Huang Z, Laliberté F, Liu S, Papp R, Nicholson DW, Young RN.
Abstract: The SAR study of a series of 6-aryloxymethyl-8-aryl substituted quinolines is described. Optimization of the series led to the discovery of compound 26b, a highly potent (IC50=0.6 nM) and selective PDE4D inhibitor with a 75-fold selectivity over the A, B, and C subtypes and over 18,000-fold selectivity against other PDE family members. Rat pharmacokinetics and tissue distribution are also summarized.
CiteXplore: 20709547