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Journal Abstract Search

86 related items for PubMed ID: 22153937

  • 1. Novel brain penetrant benzofuropiperidine 5-HT₆ receptor antagonists.
    Sundar BG, Bailey TR, Dunn DD, Bacon ER, Salvino JM, Morton GC, Aimone LD, Zeqi H, Mathiasen JR, Dicamillo A, Huffman MJ, McKenna BA, Kopec K, Lu LD, Brown R, Qian J, Angeles T, Connors T, Spais C, Holskin B, Galinis D, Duzic E, Schaffhauser H, Rosse GC.
    Bioorg Med Chem Lett; 2012 Jan 01; 22(1):120-3. PubMed ID: 22153937
    [Abstract] [Full Text] [Related]

  • 2. Design, synthesis, and pharmacological evaluation of piperidin-4-yl amino aryl sulfonamides: novel, potent, selective, orally active, and brain penetrant 5-HT₆ receptor antagonists.
    Nirogi R, Shinde A, Daulatabad A, Kambhampati R, Gudla P, Shaik M, Gampa M, Balasubramaniam S, Gangadasari P, Reballi V, Badange R, Bojja K, Subramanian R, Bhyrapuneni G, Muddana N, Jayarajan P.
    J Med Chem; 2012 Nov 08; 55(21):9255-69. PubMed ID: 23006002
    [Abstract] [Full Text] [Related]

  • 3. 4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.
    Fletcher SR, Burkamp F, Blurton P, Cheng SK, Clarkson R, O'Connor D, Spinks D, Tudge M, van Niel MB, Patel S, Chapman K, Marwood R, Shepheard S, Bentley G, Cook GP, Bristow LJ, Castro JL, Hutson PH, MacLeod AM.
    J Med Chem; 2002 Jan 17; 45(2):492-503. PubMed ID: 11784153
    [Abstract] [Full Text] [Related]

  • 4. 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 01; 22(1):186-9. PubMed ID: 22153342
    [Abstract] [Full Text] [Related]

  • 5. 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 01; 19(15):4274-9. PubMed ID: 19500982
    [Abstract] [Full Text] [Related]

  • 6. Antagonists of 5-HT₆ receptors. Substituted 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines and 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[4,3-d]pyrimidines-Synthesis and 'structure-activity' relationship.
    Ivachtchenko AV, Golovina ES, Kadieva MG, Kysil VM, Mitkin OD, Vorobiev AA, Okun I.
    Bioorg Med Chem Lett; 2012 Jul 01; 22(13):4273-80. PubMed ID: 22664127
    [Abstract] [Full Text] [Related]

  • 7. (3-Phenylsulfonylcycloalkano[e and d]pyrazolo[1,5-a]pyrimidin-2-yl)amines: potent and selective antagonists of the serotonin 5-HT6 receptor.
    Ivachtchenko AV, Dmitriev DE, Golovina ES, Kadieva MG, Koryakova AG, Kysil VM, Mitkin OD, Okun IM, Tkachenko SE, Vorobiev AA.
    J Med Chem; 2010 Jul 22; 53(14):5186-96. PubMed ID: 20560595
    [Abstract] [Full Text] [Related]

  • 8. 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 01; 19(15):4325-9. PubMed ID: 19487123
    [Abstract] [Full Text] [Related]

  • 9. Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT₆ receptor antagonist showing activity in rat social recognition test.
    Tripathy R, McHugh RJ, Bacon ER, Salvino JM, Morton GC, Aimone LD, Huang Z, Mathiasen JR, DiCamillo A, Huffman MJ, McKenna BA, Kopec K, Lu LD, Qian J, Angeles TS, Connors T, Spais C, Holskin B, Duzic E, Schaffhauser H, Rossé GC.
    Bioorg Med Chem Lett; 2012 Feb 01; 22(3):1421-6. PubMed ID: 22226656
    [Abstract] [Full Text] [Related]

  • 10. Reduction of hERG inhibitory activity in the 4-piperidinyl urea series of H3 antagonists.
    Berlin M, Lee YJ, Boyce CW, Wang Y, Aslanian R, McCormick KD, Sorota S, Williams SM, West RE, Korfmacher W.
    Bioorg Med Chem Lett; 2010 Apr 01; 20(7):2359-64. PubMed ID: 20188550
    [Abstract] [Full Text] [Related]

  • 11. Design, synthesis, and structure-activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine.
    Yoshizumi T, Miyazoe H, Ito H, Tsujita T, Takahashi H, Asai M, Ozaki S, Ohta H, Okamoto O.
    Bioorg Med Chem Lett; 2008 Jul 01; 18(13):3778-82. PubMed ID: 18515099
    [Abstract] [Full Text] [Related]

  • 12. Discovery of tetrasubstituted imidazolines as potent and selective neuropeptide Y Y5 receptor antagonists: reduced human ether-a-go-go related gene potassium channel binding affinity and potent antiobesity effect.
    Sato N, Ando M, Ishikawa S, Jitsuoka M, Nagai K, Takahashi H, Sakuraba A, Tsuge H, Kitazawa H, Iwaasa H, Mashiko S, Gomori A, Moriya R, Fujino N, Ohe T, Ishihara A, Kanatani A, Fukami T.
    J Med Chem; 2009 May 28; 52(10):3385-96. PubMed ID: 19459652
    [Abstract] [Full Text] [Related]

  • 13. Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent.
    Park JS, Im W, Choi S, Park SJ, Jung JM, Baek KS, Son HP, Sharma S, Kim IS, Jung YH.
    Eur J Med Chem; 2016 Feb 15; 109():75-88. PubMed ID: 26761776
    [Abstract] [Full Text] [Related]

  • 14. Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists.
    Trani G, Baddeley SM, Briggs MA, Chuang TT, Deeks NJ, Johnson CN, Khazragi AA, Mead TL, Medhurst AD, Milner PH, Quinn LP, Ray AM, Rivers DA, Stean TO, Stemp G, Trail BK, Witty DR.
    Bioorg Med Chem Lett; 2008 Oct 15; 18(20):5698-700. PubMed ID: 18793848
    [Abstract] [Full Text] [Related]

  • 15. Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists--Increasing selectivity over hERG.
    Meyers KM, Kim N, Méndez-Andino JL, Hu XE, Mumin RN, Klopfenstein SR, Wos JA, Mitchell MC, Paris JL, Ackley DC, Holbert JK, Mittelstadt SW, Reizes O.
    Bioorg Med Chem Lett; 2007 Feb 01; 17(3):814-8. PubMed ID: 17107791
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  • 18. 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 01; 22(1):421-6. PubMed ID: 22153347
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