524774-90-1Relevant articles and documents
Substituted 4-(2,2-Diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters
Frenette, Richard,Blouin, Marc,Brideau, Christine,Chauret, Nathalie,Ducharme, Yves,Friesen, Richard W.,Hamel, Pierre,Jones, Tom R.,Laliberte, France,Li, Chun,Masson, Paul,McAuliffe, Malia,Girard, Yves
, p. 3009 - 3013 (2007/10/03)
A detailed SAR study directed toward the optimization of pharmacokinetic parameters for analogues of L-791,943 is reported. The introduction of a soft metabolic site on this structure permitted the identification of L-826,141 as a potent phosphodiesterase type 4 (PDE4) inhibitor that is well absorbed and that presents a shorter half-life than L-791,943 in a variety of animal species. The efficacy of L-826,141 is also demonstrated in different in vivo models.