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MF498 [N-{[4-(5,9-Diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis.
Clark P, Rowland SE, Denis D, Mathieu MC, Stocco R, Poirier H, Burch J, Han Y, Audoly L, Therien AG, Xu D. Clark P, et al. Among authors: xu d. J Pharmacol Exp Ther. 2008 May;325(2):425-34. doi: 10.1124/jpet.107.134510. Epub 2008 Feb 20. J Pharmacol Exp Ther. 2008. PMID: 18287210
Structure-activity relationships and pharmacokinetic parameters of quinoline acylsulfonamides as potent and selective antagonists of the EP(4) receptor.
Burch JD, Belley M, Fortin R, Deschênes D, Girard M, Colucci J, Farand J, Therien AG, Mathieu MC, Denis D, Vigneault E, Lévesque JF, Gagné S, Wrona M, Xu D, Clark P, Rowland S, Han Y. Burch JD, et al. Among authors: xu d. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2048-54. doi: 10.1016/j.bmcl.2008.01.103. Epub 2008 Jan 31. Bioorg Med Chem Lett. 2008. PMID: 18291643
The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.
Blouin M, Han Y, Burch J, Farand J, Mellon C, Gaudreault M, Wrona M, Lévesque JF, Denis D, Mathieu MC, Stocco R, Vigneault E, Therien A, Clark P, Rowland S, Xu D, O'Neill G, Ducharme Y, Friesen R. Blouin M, et al. Among authors: xu d. J Med Chem. 2010 Mar 11;53(5):2227-38. doi: 10.1021/jm901771h. J Med Chem. 2010. PMID: 20163116
Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain.
Colucci J, Boyd M, Berthelette C, Chiasson JF, Wang Z, Ducharme Y, Friesen R, Wrona M, Levesque JF, Denis D, Mathieu MC, Stocco R, Therien AG, Clarke P, Rowland S, Xu D, Han Y. Colucci J, et al. Among authors: xu d. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3760-3. doi: 10.1016/j.bmcl.2010.04.065. Epub 2010 Apr 18. Bioorg Med Chem Lett. 2010. PMID: 20471829
Naphthalene/quinoline amides and sulfonylureas as potent and selective antagonists of the EP4 receptor.
Burch JD, Farand J, Colucci J, Sturino C, Ducharme Y, Friesen RW, Lévesque JF, Gagné S, Wrona M, Therien AG, Mathieu MC, Denis D, Vigneault E, Xu D, Clark P, Rowland S, Han Y. Burch JD, et al. Among authors: xu d. Bioorg Med Chem Lett. 2011 Feb 1;21(3):1041-6. doi: 10.1016/j.bmcl.2010.12.014. Epub 2010 Dec 8. Bioorg Med Chem Lett. 2011. PMID: 21215624
Trisubstituted ureas as potent and selective mPGES-1 inhibitors.
Chiasson JF, Boulet L, Brideau C, Chau A, Claveau D, Côté B, Ethier D, Giroux A, Guay J, Guiral S, Mancini J, Massé F, Méthot N, Riendeau D, Roy P, Rubin J, Xu D, Yu H, Ducharme Y, Friesen RW. Chiasson JF, et al. Among authors: xu d. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1488-92. doi: 10.1016/j.bmcl.2011.01.006. Epub 2011 Jan 13. Bioorg Med Chem Lett. 2011. PMID: 21295979
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
Giroux A, Boulet L, Brideau C, Chau A, Claveau D, Côté B, Ethier D, Frenette R, Gagnon M, Guay J, Guiral S, Mancini J, Martins E, Massé F, Méthot N, Riendeau D, Rubin J, Xu D, Yu H, Ducharme Y, Friesen RW. Giroux A, et al. Among authors: xu d. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5837-41. doi: 10.1016/j.bmcl.2009.08.085. Epub 2009 Aug 28. Bioorg Med Chem Lett. 2009. PMID: 19748780
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
Côté B, Boulet L, Brideau C, Claveau D, Ethier D, Frenette R, Gagnon M, Giroux A, Guay J, Guiral S, Mancini J, Martins E, Massé F, Méthot N, Riendeau D, Rubin J, Xu D, Yu H, Ducharme Y, Friesen RW. Côté B, et al. Among authors: xu d. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6816-20. doi: 10.1016/j.bmcl.2007.10.033. Epub 2007 Oct 17. Bioorg Med Chem Lett. 2007. PMID: 18029174
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