1252807-75-2Relevant academic research and scientific papers
The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors
Aspiotis, Renee,Deschênes, Denis,Dubé, Daniel,Girard, Yves,Huang, Zheng,Laliberté, France,Liu, Susana,Papp, Robert,Nicholson, Donald W.,Young, Robert N.
scheme or table, p. 5502 - 5505 (2010/12/24)
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.
