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Page 1
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.
Macdonald D, Mastracchio A, Perrier H, Dubé D, Gallant M, Lacombe P, Deschênes D, Roy B, Scheigetz J, Bateman K, Li C, Trimble LA, Day S, Chauret N, Nicoll-Griffith DA, Silva JM, Huang Z, Laliberté F, Liu S, Ethier D, Pon D, Muise E, Boulet L, Chan CC, Styhler A, Charleson S, Mancini J, Masson P, Claveau D, Nicholson D, Turner M, Young RN, Girard Y. Macdonald D, et al. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5241-6. doi: 10.1016/j.bmcl.2005.08.036. Epub 2005 Sep 15. Bioorg Med Chem Lett. 2005. PMID: 16168647
Design, synthesis, and biological evaluation of 8-biarylquinolines: a novel class of PDE4 inhibitors.
Gallant M, Chauret N, Claveau D, Day S, Deschênes D, Dubé D, Huang Z, Lacombe P, Laliberté F, Lévesque JF, Liu S, Macdonald D, Mancini J, Masson P, Mastracchio A, Nicholson D, Nicoll-Griffith DA, Perrier H, Salem M, Styhler A, Young RN, Girard Y. Gallant M, et al. Among authors: nicoll griffith da. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1407-12. doi: 10.1016/j.bmcl.2008.01.004. Epub 2008 Jan 8. Bioorg Med Chem Lett. 2008. PMID: 18207397
Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors.
Lacombe P, Chauret N, Claveau D, Day S, Deschênes D, Dubé D, Gallant M, Girard Y, Huang Z, Laliberté F, Lévesque JF, Liu S, Macdonald D, Mancini JA, Masson P, Nicholson DW, Nicoll-Griffith DA, Salem M, Styhler A, Young RN. Lacombe P, et al. Among authors: nicoll griffith da. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5266-9. doi: 10.1016/j.bmcl.2009.03.105. Epub 2009 Mar 26. Bioorg Med Chem Lett. 2009. PMID: 19640717
Dioxabicyclooctanyl naphthalenenitriles as nonredox 5-lipoxygenase inhibitors: structure-activity relationship study directed toward the improvement of metabolic stability.
Delorme D, Ducharme Y, Brideau C, Chan CC, Chauret N, Desmarais S, Dubé D, Falgueyret JP, Fortin R, Guay J, Hamel P, Jones TR, Lépine C, Li C, McAuliffe M, McFarlane CS, Nicoll-Griffith DA, Riendeau D, Yergey JA, Girard Y. Delorme D, et al. J Med Chem. 1996 Sep 27;39(20):3951-70. doi: 10.1021/jm960301c. J Med Chem. 1996. PMID: 8831761
Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).
Sturino CF, O'Neill G, Lachance N, Boyd M, Berthelette C, Labelle M, Li L, Roy B, Scheigetz J, Tsou N, Aubin Y, Bateman KP, Chauret N, Day SH, Lévesque JF, Seto C, Silva JH, Trimble LA, Carriere MC, Denis D, Greig G, Kargman S, Lamontagne S, Mathieu MC, Sawyer N, Slipetz D, Abraham WM, Jones T, McAuliffe M, Piechuta H, Nicoll-Griffith DA, Wang Z, Zamboni R, Young RN, Metters KM. Sturino CF, et al. J Med Chem. 2007 Feb 22;50(4):794-806. doi: 10.1021/jm0603668. J Med Chem. 2007. PMID: 17300164
58 results