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Items: 1 to 20 of 102

1.

Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.

Coon T, Moree WJ, Li B, Yu J, Zamani-Kord S, Malany S, Santos MA, Hernandez LM, Petroski RE, Sun A, Wen J, Sullivan S, Haelewyn J, Hedrick M, Hoare SJ, Bradbury MJ, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4380-4. doi: 10.1016/j.bmcl.2009.05.086. Epub 2009 May 27.

PMID:
19553115
2.

The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia.

Lavrador-Erb K, Ravula SB, Yu J, Zamani-Kord S, Moree WJ, Petroski RE, Wen J, Malany S, Hoare SR, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2010 May 1;20(9):2916-9. doi: 10.1016/j.bmcl.2010.03.027. Epub 2010 Mar 10.

PMID:
20347297
3.

Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H₁-antihistamines for insomnia.

Ravula SB, Yu J, Tran JA, Arellano M, Tucci FC, Moree WJ, Li BF, Petroski RE, Wen J, Malany S, Hoare SR, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):421-6. doi: 10.1016/j.bmcl.2011.10.115. Epub 2011 Nov 15.

PMID:
22153347
4.

2,4-Diaminopyridine delta-opioid receptor agonists and their associated hERG pharmacology.

Owen DR, Rodriguez-Lens M, Corless MD, Gaulier SM, Horne VA, Kinloch RA, Maw GN, Pearce DW, Rees H, Ringer TJ, Ryckmans T, Stammen BL.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1702-6. doi: 10.1016/j.bmcl.2009.01.106. Epub 2009 Feb 5.

PMID:
19231185
5.

Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.

Moree WJ, Li BF, Jovic F, Coon T, Yu J, Gross RS, Tucci F, Marinkovic D, Zamani-Kord S, Malany S, Bradbury MJ, Hernandez LM, O'Brien Z, Wen J, Wang H, Hoare SR, Petroski RE, Sacaan A, Madan A, Crowe PD, Beaton G.

J Med Chem. 2009 Sep 10;52(17):5307-10. doi: 10.1021/jm900933k.

PMID:
19663387
6.

Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists.

Sasaki T, Takahashi T, Nagase T, Mizutani T, Ito S, Mitobe Y, Miyamoto Y, Kanesaka M, Yoshimoto R, Tanaka T, Takenaga N, Tokita S, Sato N.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4232-6. doi: 10.1016/j.bmcl.2009.05.101. Epub 2009 May 30.

PMID:
19520574
7.

Optimization of a series of 2,4-diaminopyridines as neuropeptide Y Y1 receptor antagonists with reduced hERG activity.

Kameda M, Kobayashi K, Ito H, Miyazoe H, Tsujino T, Nakama C, Kawamoto H, Ando M, Ito S, Suzuki T, Kanno T, Tanaka T, Tahara Y, Tani T, Tanaka S, Tokita S, Sato N.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4325-9. doi: 10.1016/j.bmcl.2009.05.069. Epub 2009 May 24.

PMID:
19487123
8.

Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists.

Becknell NC, Dandu RR, Lyons JA, Aimone LD, Raddatz R, Hudkins RL.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):186-9. doi: 10.1016/j.bmcl.2011.11.038. Epub 2011 Nov 16.

PMID:
22153342
9.

Synthesis, biological activity, QSAR and QSPR study of 2-aminobenzimidazole derivatives as potent H3-antagonists.

Mor M, Bordi F, Silva C, Rivara S, Zuliani V, Vacondio F, Rivara M, Barocelli E, Bertoni S, Ballabeni V, Magnanini F, Impicciatore M, Plazzi PV.

Bioorg Med Chem. 2004 Feb 15;12(4):663-74.

PMID:
14759727
10.

Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.

Li BF, Moree WJ, Yu J, Coon T, Zamani-Kord S, Malany S, Jalali K, Wen J, Wang H, Yang C, Hoare SR, Petroski RE, Madan A, Crowe PD, Beaton G.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2629-33. doi: 10.1016/j.bmcl.2010.02.055. Epub 2010 Feb 18.

PMID:
20227880
11.

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.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):71-5. doi: 10.1016/j.bmcl.2011.11.075. Epub 2011 Nov 30.

PMID:
22172695
12.

Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor.

Guay D, Boulet L, Friesen RW, Girard M, Hamel P, Huang Z, Laliberté F, Laliberté S, Mancini JA, Muise E, Pon D, Styhler A.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5554-8. doi: 10.1016/j.bmcl.2008.09.009. Epub 2008 Sep 6.

PMID:
18835163
13.

The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity.

Siu T, Li Y, Nagasawa J, Liang J, Tehrani L, Chua P, Jones RE, Defeo-Jones D, Barnett SF, Robinson RG.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4191-4. doi: 10.1016/j.bmcl.2008.05.084. Epub 2008 May 24.

PMID:
18550373
14.

Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution.

Blum CA, Zheng X, Brielmann H, Hodgetts KJ, Bakthavatchalam R, Chandrasekhar J, Krause JE, Cortright D, Matson D, Crandall M, Ngo CK, Fung L, Day M, Kershaw M, De Lombaert S, Chenard BL.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4573-7. doi: 10.1016/j.bmcl.2008.07.036. Epub 2008 Jul 15.

PMID:
18662872
15.

4-phenoxypiperidines: potent, conformationally restricted, non-imidazole histamine H3 antagonists.

Dvorak CA, Apodaca R, Barbier AJ, Berridge CW, Wilson SJ, Boggs JD, Xiao W, Lovenberg TW, Carruthers NI.

J Med Chem. 2005 Mar 24;48(6):2229-38.

PMID:
15771465
16.
17.

Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity.

Kobayashi K, Kato T, Yamamoto I, Shimizu A, Mizutani S, Asai M, Kawamoto H, Ito S, Yoshizumi T, Hirayama M, Ozaki S, Ohta H, Okamoto O.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):3100-3. doi: 10.1016/j.bmcl.2009.04.022. Epub 2009 Apr 11.

PMID:
19398200
18.

Optimization of 2-piperidin-4-yl-acetamides as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Designing out hERG inhibition.

Berglund S, Egner BJ, Gradén H, Gradén J, Morgan DG, Inghardt T, Giordanetto F.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4268-73. doi: 10.1016/j.bmcl.2009.05.067. Epub 2009 May 24.

PMID:
19500979
19.

Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors.

Letavic MA, Stocking EM, Barbier AJ, Bonaventure P, Boggs JD, Lord B, Miller KL, Wilson SJ, Carruthers NI.

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4799-803. Epub 2007 Jun 26.

PMID:
17616397
20.

Optimization of piperidin-4-yl-urea-containing melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Reducing hERG-associated liabilities.

Berglund S, Egner BJ, Gradén H, Gradén J, Morgan DG, Inghardt T, Giordanetto F.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4274-9. doi: 10.1016/j.bmcl.2009.05.066. Epub 2009 May 27.

PMID:
19500982

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