Author/Authors :
Richard Frenette، نويسنده , , Marc Blouin، نويسنده , , Christine Brideau، نويسنده , , Nathalie Chauret، نويسنده , , Yves Ducharme، نويسنده , , Richard W. Friesen، نويسنده , , Pierre Hamel، نويسنده , , Tom R. Jones، نويسنده , , France Laliberté، نويسنده , , Chun Li، نويسنده , , Paul Masson، نويسنده , , Malia McAuliffe، نويسنده , , Jean-Yves Girard، نويسنده ,
Abstract :
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.
