2. Academic Validation
  3. Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters

Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters

  • Bioorg Med Chem Lett. 2002 Oct 21;12(20):3009-13. doi: 10.1016/s0960-894x(02)00615-7.
Richard Frenette 1,  Marc Blouin,  Christine Brideau,  Nathalie Chauret,  Yves Ducharme,  Richard W Friesen,  Pierre Hamel,  Tom R Jones,  France Laliberté,  Chun Li,  Paul Masson,  Malia McAuliffe,  Yves Girard
Affiliations

Affiliation

  • 1 Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe-Claire-Dorval, Québec, Canada. richard_frenette@merck.com
PMID: 12270195 DOI: 10.1016/s0960-894x(02)00615-7
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.

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