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Items: 1 to 20 of 115

1.

N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist.

Hirose M, Egashira S, Goto Y, Hashihayata T, Ohtake N, Iwaasa H, Hata M, Fukami T, Kanatani A, Yamada K.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4497-9.

PMID:
14643355
2.

Discovery of dual orexin receptor antagonists (DORAs) for the treatment of insomnia.

Coleman PJ, Cox CD, Roecker AJ.

Curr Top Med Chem. 2011;11(6):696-725. Review.

PMID:
21261591
3.

Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor.

Perrey DA, German NA, Gilmour BP, Li JX, Harris DL, Thomas BF, Zhang Y.

J Med Chem. 2013 Sep 12;56(17):6901-16. doi: 10.1021/jm400720h. Epub 2013 Aug 26.

4.

Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.

McAtee LC, Sutton SW, Rudolph DA, Li X, Aluisio LE, Phuong VK, Dvorak CA, Lovenberg TW, Carruthers NI, Jones TK.

Bioorg Med Chem Lett. 2004 Aug 16;14(16):4225-9.

PMID:
15261275
5.

Proline bis-amides as potent dual orexin receptor antagonists.

Bergman JM, Roecker AJ, Mercer SP, Bednar RA, Reiss DR, Ransom RW, Meacham Harrell C, Pettibone DJ, Lemaire W, Murphy KL, Li C, Prueksaritanont T, Winrow CJ, Renger JJ, Koblan KS, Hartman GD, Coleman PJ.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1425-30. doi: 10.1016/j.bmcl.2008.01.001. Epub 2008 Jan 8.

PMID:
18207395
6.

Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B.

Asahi S, Egashira S, Matsuda M, Iwaasa H, Kanatani A, Ohkubo M, Ihara M, Morishima H.

Bioorg Med Chem Lett. 2003 Jan 6;13(1):111-3.

PMID:
12467628
7.

Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats.

Whitman DB, Cox CD, Breslin MJ, Brashear KM, Schreier JD, Bogusky MJ, Bednar RA, Lemaire W, Bruno JG, Hartman GD, Reiss DR, Harrell CM, Kraus RL, Li Y, Garson SL, Doran SM, Prueksaritanont T, Li C, Winrow CJ, Koblan KS, Renger JJ, Coleman PJ.

ChemMedChem. 2009 Jul;4(7):1069-74. doi: 10.1002/cmdc.200900069.

PMID:
19418500
8.

Synthesis, structure-activity relationship studies, and identification of novel 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 1.

Sifferlen T, Koberstein R, Cottreel E, Boller A, Weller T, Gatfield J, Brisbare-Roch C, Jenck F, Boss C.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2212-6. doi: 10.1016/j.bmcl.2013.01.088. Epub 2013 Jan 29.

PMID:
23434414
9.

Orexin receptor antagonists: medicinal chemistry and therapeutic potential.

Roecker AJ, Coleman PJ.

Curr Top Med Chem. 2008;8(11):977-87. Review.

PMID:
18673167
10.

Effect of 1-substitution on tetrahydroisoquinolines as selective antagonists for the orexin-1 receptor.

Perrey DA, German NA, Decker AM, Thorn D, Li JX, Gilmour BP, Thomas BF, Harris DL, Runyon SP, Zhang Y.

ACS Chem Neurosci. 2015 Apr 15;6(4):599-614. doi: 10.1021/cn500330v. Epub 2015 Feb 12.

11.

Synthesis, resolution, stereochemistry, and molecular modeling of (R)- and (S)-2-acetyl-1-(4'-chlorophenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline AMPAR antagonists.

Gitto R, Ficarra R, Stancanelli R, Guardo M, De Luca L, Barreca ML, Pagano B, Rotondo A, Bruno G, Russo E, De Sarro G, Chimirri A.

Bioorg Med Chem. 2007 Aug 15;15(16):5417-23. Epub 2007 May 31.

PMID:
17566746
12.

Synthesis and SAR of novel histamine H3 receptor antagonists.

Jesudason CD, Beavers LS, Cramer JW, Dill J, Finley DR, Lindsley CW, Stevens FC, Gadski RA, Oldham SW, Pickard RT, Siedem CS, Sindelar DK, Singh A, Watson BM, Hipskind PA.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3415-8. Epub 2006 May 3.

PMID:
16677814
14.

Synthesis and anticonvulsant properties of tetrahydroisoquinoline derivatives.

Gitto R, Caruso R, Orlando V, Quartarone S, Barreca ML, Ferreri G, Russo E, De Sarro G, Chimirri A.

Farmaco. 2004 Jan;59(1):7-12.

PMID:
14751310
15.

Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.

Di Fabio R, Pellacani A, Faedo S, Roth A, Piccoli L, Gerrard P, Porter RA, Johnson CN, Thewlis K, Donati D, Stasi L, Spada S, Stemp G, Nash D, Branch C, Kindon L, Massagrande M, Poffe A, Braggio S, Chiarparin E, Marchioro C, Ratti E, Corsi M.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7. doi: 10.1016/j.bmcl.2011.06.086. Epub 2011 Jun 30.

PMID:
21831639
16.

N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists.

Aissaoui H, Koberstein R, Zumbrunn C, Gatfield J, Brisbare-Roch C, Jenck F, Treiber A, Boss C.

Bioorg Med Chem Lett. 2008 Nov 1;18(21):5729-33. doi: 10.1016/j.bmcl.2008.09.079. Epub 2008 Sep 26.

PMID:
18845436
17.
18.

1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.

Porter RA, Chan WN, Coulton S, Johns A, Hadley MS, Widdowson K, Jerman JC, Brough SJ, Coldwell M, Smart D, Jewitt F, Jeffrey P, Austin N.

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1907-10.

PMID:
11459658
19.

Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.

Renaud J, Bischoff SF, Buhl T, Floersheim P, Fournier B, Geiser M, Halleux C, Kallen J, Keller H, Ramage P.

J Med Chem. 2005 Jan 27;48(2):364-79.

PMID:
15658851
20.
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