Substituted aminopyridines as potent and selective phosphodiesterase-4 inhibitors

…, RW Friesen, F Laliberté, P Masson, A Styhler…

文献索引：Cote, Bernard; Frenette, Richard; Prescott, Sylvie; Blouin, Marc; Brideau, Christine; Ducharme, Yves; Friesen, Richard W.; Laliberte, France; Masson, Paul; Styhler, Angela; Girard, Yves Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 4 p. 741 - 744

全文：HTML全文

被引用次数: 4

摘要

The synthesis and the biological evaluation of new potent phosphodiesterase type 4 (PDE4) inhibitors are presented. This new series was elaborated by replacement of the metabolically resistant phenyl hexafluorocarbinol of L-791,943 (1) by a substituted aminopyridine residue. The structure–activity relationship of N-substitution on 3 led to the identification of (−)-3n which exhibited a good PDE4 inhibitor activity (HWB-TNFα= 0.12 ...