Substituted aminopyridines as potent and selective phosphodiesterase-4 inhibitors
…, RW Friesen, F Laliberté, P Masson, A Styhler…
Index: 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
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Citation Number: 4
Abstract
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 ...
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[Friesen, Richard W.; Ducharme, Yves; Ball, Richard G.; Blouin, Marc; Boulet, Louise; Cote, Bernard; Frenette, Richard; Girard, Mario; Guay, Daniel; Huang, Zheng; Jones, Thomas R.; Laliberte, France; Lynch, Joseph J.; Mancini, Joseph; Martins, Evelyn; Masson, Paul; Muise, Eric; Pon, Douglas J.; Siegl, Peter K. S.; Styhler, Angela; Tsou, Nancy N.; Turner, Mervyn J.; Young, Robert N.; Girardt, Yves Journal of Medicinal Chemistry, 2003 , vol. 46, # 12 p. 2413 - 2426]
[Friesen, Richard W.; Ducharme, Yves; Ball, Richard G.; Blouin, Marc; Boulet, Louise; Cote, Bernard; Frenette, Richard; Girard, Mario; Guay, Daniel; Huang, Zheng; Jones, Thomas R.; Laliberte, France; Lynch, Joseph J.; Mancini, Joseph; Martins, Evelyn; Masson, Paul; Muise, Eric; Pon, Douglas J.; Siegl, Peter K. S.; Styhler, Angela; Tsou, Nancy N.; Turner, Mervyn J.; Young, Robert N.; Girardt, Yves Journal of Medicinal Chemistry, 2003 , vol. 46, # 12 p. 2413 - 2426]