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Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).
Le Bourdonnec B, Windh RT, Leister LK, Zhou QJ, Ajello CW, Gu M, Chu GH, Tuthill PA, Barker WM, Koblish M, Wiant DD, Graczyk TM, Belanger S, Cassel JA, Feschenko MS, Brogdon BL, Smith SA, Derelanko MJ, Kutz S, Little PJ, DeHaven RN, DeHaven-Hudkins DL, Dolle RE. Le Bourdonnec B, et al. Among authors: smith sa. J Med Chem. 2009 Sep 24;52(18):5685-702. doi: 10.1021/jm900773n. J Med Chem. 2009. PMID: 19694468
Novel pyridine derivatives as potent and selective CB2 cannabinoid receptor agonists.
Chu GH, Saeui CT, Worm K, Weaver DG, Goodman AJ, Broadrup RL, Cassel JA, DeHaven RN, LaBuda CJ, Koblish M, Brogdon B, Smith S, Le Bourdonnec B, Dolle RE. Chu GH, et al. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5931-5. doi: 10.1016/j.bmcl.2009.08.063. Epub 2009 Aug 21. Bioorg Med Chem Lett. 2009. PMID: 19736007
Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
Le Bourdonnec B, Windh RT, Ajello CW, Leister LK, Gu M, Chu GH, Tuthill PA, Barker WM, Koblish M, Wiant DD, Graczyk TM, Belanger S, Cassel JA, Feschenko MS, Brogdon BL, Smith SA, Christ DD, Derelanko MJ, Kutz S, Little PJ, DeHaven RN, DeHaven-Hudkins DL, Dolle RE. Le Bourdonnec B, et al. Among authors: smith sa. J Med Chem. 2008 Oct 9;51(19):5893-6. doi: 10.1021/jm8008986. Epub 2008 Sep 13. J Med Chem. 2008. PMID: 18788723
CB2 selective sulfamoyl benzamides: optimization of the amide functionality.
Goodman AJ, Ajello CW, Worm K, Le Bourdonnec B, Savolainen MA, O'Hare H, Cassel JA, Stabley GJ, Dehaven RN, Labuda CJ, Koblish M, Little PJ, Brogdon BL, Smith SA, Dolle RE. Goodman AJ, et al. Among authors: smith sa. Bioorg Med Chem Lett. 2009 Jan 15;19(2):309-13. doi: 10.1016/j.bmcl.2008.11.091. Epub 2008 Nov 27. Bioorg Med Chem Lett. 2009. PMID: 19091565
Discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB2 agonists.
Worm K, Weaver DG, Green RC, Saeui CT, Dulay DM, Barker WM, Cassel JA, Stabley GJ, DeHaven RN, LaBuda CJ, Koblish M, Brogdon BL, Smith SA, Dolle RE. Worm K, et al. Among authors: smith sa. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5004-8. doi: 10.1016/j.bmcl.2009.07.057. Epub 2009 Jul 12. Bioorg Med Chem Lett. 2009. PMID: 19646869
Novel sulfamoyl benzamides as selective CB(2) agonists with improved in vitro metabolic stability.
Sellitto I, Le Bourdonnec B, Worm K, Goodman A, Savolainen MA, Chu GH, Ajello CW, Saeui CT, Leister LK, Cassel JA, Dehaven RN, Labuda CJ, Koblish M, Little PJ, Brogdon BL, Smith SA, Dolle RE. Sellitto I, et al. Among authors: smith sa. Bioorg Med Chem Lett. 2010 Jan 1;20(1):387-91. doi: 10.1016/j.bmcl.2009.10.062. Epub 2009 Oct 17. Bioorg Med Chem Lett. 2010. PMID: 19919895
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
Lopez FJ, Arias L, Chan R, Clarke DE, Elworthy TR, Ford AP, Guzman A, Jaime-Figueroa S, Jasper JR, Morgans DJ Jr, Padilla F, Perez-Medrano A, Quintero C, Romero M, Sandoval L, Smith SA, Williams TJ, Blue DR. Lopez FJ, et al. Among authors: smith sa. Bioorg Med Chem Lett. 2003 Jun 2;13(11):1873-8. doi: 10.1016/s0960-894x(03)00305-6. Bioorg Med Chem Lett. 2003. PMID: 12749888
1,650 results