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Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors.
Bioorg Med Chem Lett 2003; 13(11):1923-6BM

Abstract

The synthesis and the phosphodiesterase-4 (PDE4) inhibitory activity of 2-pyridinemethanol derivatives is described. The evaluation of the structure-activity relationship (SAR) in this series of novel PDE4 inhibitors led to the identification of compound 9 which exhibits excellent in vitro activity, desirable pharmacokinetic parameters and good efficacy in animal models of bronchoconstriction.

Authors+Show Affiliations

Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire-Dorval, Québec, Canada H9R 4P8. yves_ducharme@merck.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

12749899

Citation

Ducharme, Yves, et al. "Substituted 2-pyridinemethanol Derivatives as Potent and Selective Phosphodiesterase-4 Inhibitors." Bioorganic & Medicinal Chemistry Letters, vol. 13, no. 11, 2003, pp. 1923-6.
Ducharme Y, Friesen RW, Blouin M, et al. Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors. Bioorg Med Chem Lett. 2003;13(11):1923-6.
Ducharme, Y., Friesen, R. W., Blouin, M., Côté, B., Dubé, D., Ethier, D., ... Girard, Y. (2003). Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors. Bioorganic & Medicinal Chemistry Letters, 13(11), pp. 1923-6.
Ducharme Y, et al. Substituted 2-pyridinemethanol Derivatives as Potent and Selective Phosphodiesterase-4 Inhibitors. Bioorg Med Chem Lett. 2003 Jun 2;13(11):1923-6. PubMed PMID: 12749899.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors. AU - Ducharme,Yves, AU - Friesen,Richard W, AU - Blouin,Marc, AU - Côté,Bernard, AU - Dubé,Daniel, AU - Ethier,Diane, AU - Frenette,Richard, AU - Laliberté,France, AU - Mancini,Joseph A, AU - Masson,Paul, AU - Styhler,Angela, AU - Young,Robert N, AU - Girard,Yves, PY - 2003/5/17/pubmed PY - 2004/2/18/medline PY - 2003/5/17/entrez SP - 1923 EP - 6 JF - Bioorganic & medicinal chemistry letters JO - Bioorg. Med. Chem. Lett. VL - 13 IS - 11 N2 - The synthesis and the phosphodiesterase-4 (PDE4) inhibitory activity of 2-pyridinemethanol derivatives is described. The evaluation of the structure-activity relationship (SAR) in this series of novel PDE4 inhibitors led to the identification of compound 9 which exhibits excellent in vitro activity, desirable pharmacokinetic parameters and good efficacy in animal models of bronchoconstriction. SN - 0960-894X UR - https://www.unboundmedicine.com/medline/citation/12749899/Substituted_2_pyridinemethanol_derivatives_as_potent_and_selective_phosphodiesterase_4_inhibitors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960894X03003147 DB - PRIME DP - Unbound Medicine ER -