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Page 1
Design and evaluation of novel biphenyl sulfonamide derivatives with potent histamine H(3) receptor inverse agonist activity.
Covel JA, Santora VJ, Smith JM, Hayashi R, Gallardo C, Weinhouse MI, Ibarra JB, Schultz JA, Park DM, Estrada SA, Hofilena BJ, Pulley MD, Smith BM, Ren A, Suarez M, Frazer J, Edwards J, Hauser EK, Lorea J, Semple G, Grottick AJ. Covel JA, et al. Among authors: semple g. J Med Chem. 2009 Sep 24;52(18):5603-11. doi: 10.1021/jm900857n. J Med Chem. 2009. PMID: 19722526
A new family of H3 receptor antagonists based on the natural product Conessine.
Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Sengupta D, Duffield JJ, Semple G, Webb RR, Sage C, Ren A, Pereira G, Knudsen J, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Whelan K, Grottick AJ. Santora VJ, et al. Among authors: semple g. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1490-4. doi: 10.1016/j.bmcl.2007.12.059. Epub 2007 Dec 25. Bioorg Med Chem Lett. 2008. PMID: 18194865
Novel H3 receptor antagonists with improved pharmacokinetic profiles.
Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Semple G, Ren A, Pereira G, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Lorea J, Grottick AJ. Santora VJ, et al. Among authors: semple g. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4133-6. doi: 10.1016/j.bmcl.2008.05.086. Epub 2008 May 24. Bioorg Med Chem Lett. 2008. PMID: 18554904
Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia.
Xiong Y, Ullman B, Choi JS, Cherrier M, Strah-Pleynet S, Decaire M, Dosa PI, Feichtinger K, Teegarden BR, Frazer JM, Yoon WH, Shan Y, Whelan K, Hauser EK, Grottick AJ, Semple G, Al-Shamma H. Xiong Y, et al. Among authors: semple g. J Med Chem. 2010 Aug 12;53(15):5696-706. doi: 10.1021/jm100479q. J Med Chem. 2010. PMID: 20684606
Identification of biaryl sulfone derivatives as antagonists of the histamine H₃ receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916).
Semple G, Santora VJ, Smith JM, Covel JA, Hayashi R, Gallardo C, Ibarra JB, Schultz JA, Park DM, Estrada SA, Hofilena BJ, Smith BM, Ren A, Suarez M, Frazer J, Edwards JE, Hart R, Hauser EK, Lorea J, Grottick AJ. Semple G, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):71-5. doi: 10.1016/j.bmcl.2011.11.075. Epub 2011 Nov 30. Bioorg Med Chem Lett. 2012. PMID: 22172695
Identification of fused bicyclic heterocycles as potent and selective 5-HT(2A) receptor antagonists for the treatment of insomnia.
Xiong Y, Ullman B, Choi JS, Cherrier M, Strah-Pleynet S, Decaire M, Feichtinger K, Frazer JM, Yoon WH, Whelan K, Sanabria EK, Grottick AJ, Al-Shamma H, Semple G. Xiong Y, et al. Among authors: semple g. Bioorg Med Chem Lett. 2012 Mar 1;22(5):1870-3. doi: 10.1016/j.bmcl.2012.01.080. Epub 2012 Jan 28. Bioorg Med Chem Lett. 2012. PMID: 22325948
Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis.
Xiong Y, Teegarden BR, Choi JS, Strah-Pleynet S, Decaire M, Jayakumar H, Dosa PI, Casper MD, Pham L, Feichtinger K, Ullman B, Adams J, Yuskin D, Frazer J, Morgan M, Sadeque A, Chen W, Webb RR, Connolly DT, Semple G, Al-Shamma H. Xiong Y, et al. Among authors: semple g. J Med Chem. 2010 Jun 10;53(11):4412-21. doi: 10.1021/jm100044a. J Med Chem. 2010. PMID: 20455563
Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Semple G, Ren A, Fioravanti B, Pereira G, Calderon I, Choi K, Xiong Y, Shin YJ, Gharbaoui T, Sage CR, Morgan M, Xing C, Chu ZL, Leonard JN, Grottick AJ, Al-Shamma H, Liang Y, Demarest KT, Jones RM. Semple G, et al. Bioorg Med Chem Lett. 2011 May 15;21(10):3134-41. doi: 10.1016/j.bmcl.2011.03.007. Epub 2011 Mar 13. Bioorg Med Chem Lett. 2011. PMID: 21444206
81 results