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Page 1
Comparison between two classes of selective EP(3) antagonists and their biological activities.
Belley M, Chan CC, Gareau Y, Gallant M, Juteau H, Houde K, Lachance N, Labelle M, Sawyer N, Tremblay N, Lamontagne S, Carrière MC, Denis D, Greig GM, Slipetz D, Gordon R, Chauret N, Li C, Zamboni RJ, Metters KM. Belley M, et al. Among authors: chauret n. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5639-42. doi: 10.1016/j.bmcl.2006.08.025. Epub 2006 Aug 22. Bioorg Med Chem Lett. 2006. PMID: 16931013
Two different series of very potent and selective EP(3) antagonists have been reported: a novel series of ortho-substituted cinnamic acids [Belley, M., Gallant, M., Roy, B., Houde, K., Lachance, N., Labelle, M., Trimble, L., Chauret, N., Li, C., Sawyer, N …
Two different series of very potent and selective EP(3) antagonists have been reported: a novel series of ortho-substituted cinnamic acids [ …
Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP(3) antagonists.
Belley M, Gallant M, Roy B, Houde K, Lachance N, Labelle M, Trimble LA, Chauret N, Li C, Sawyer N, Tremblay N, Lamontagne S, Carrière MC, Denis D, Greig GM, Slipetz D, Metters KM, Gordon R, Chan CC, Zamboni RJ. Belley M, et al. Among authors: chauret n. Bioorg Med Chem Lett. 2005 Feb 1;15(3):527-30. doi: 10.1016/j.bmcl.2004.11.051. Bioorg Med Chem Lett. 2005. PMID: 15664806
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. Among authors: chauret n. J Med Chem. 2007 Feb 22;50(4):794-806. doi: 10.1021/jm0603668. J Med Chem. 2007. PMID: 17300164
Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile.
Leblanc Y, Roy P, Wang Z, Li CS, Chauret N, Nicoll-Griffith DA, Silva JM, Aubin Y, Yergey JA, Chan CC, Riendeau D, Brideau C, Gordon R, Xu L, Webb J, Visco DM, Prasit P. Leblanc Y, et al. Among authors: chauret n. Bioorg Med Chem Lett. 2002 Nov 18;12(22):3317-20. doi: 10.1016/s0960-894x(02)00739-4. Bioorg Med Chem Lett. 2002. PMID: 12392741
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. Among authors: chauret n. 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
In vitro biotransformations of the prostaglandin D2 (DP) antagonist MK-0524 and synthesis of metabolites.
Nicoll-Griffith DA, Seto C, Aubin Y, Lévesque JF, Chauret N, Day S, Silva JM, Trimble LA, Truchon JF, Berthelette C, Lachance N, Wang Z, Sturino C, Braun M, Zamboni R, Young RN. Nicoll-Griffith DA, et al. Among authors: chauret n. Bioorg Med Chem Lett. 2007 Jan 15;17(2):301-4. doi: 10.1016/j.bmcl.2006.10.055. Epub 2006 Oct 25. Bioorg Med Chem Lett. 2007. PMID: 17095220
Metabolic activation of indole-containing prostaglandin D2 receptor 1 antagonists: impacts of glutathione trapping and glucuronide conjugation on covalent binding.
Lévesque JF, Day SH, Chauret N, Seto C, Trimble L, Bateman KP, Silva JM, Berthelette C, Lachance N, Boyd M, Li L, Sturino CF, Wang Z, Zamboni R, Young RN, Nicoll-Griffith DA. Lévesque JF, et al. Among authors: chauret n. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3038-43. doi: 10.1016/j.bmcl.2007.03.058. Epub 2007 Mar 23. Bioorg Med Chem Lett. 2007. PMID: 17418572
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: chauret n. 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
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Kimmel DB, Lamontagne S, Léger S, LeRiche T, Li CS, Massé F, McKay DJ, Nicoll-Griffith DA, Oballa RM, Palmer JT, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Venuti MC, Wesolowski G, Young RN, Zamboni R, Black WC. Gauthier JY, et al. Among authors: chauret n. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. doi: 10.1016/j.bmcl.2007.12.047. Epub 2008 Jan 15. Bioorg Med Chem Lett. 2008. PMID: 18226527
61 results