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Items: 1 to 20 of 102

1.

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.

PMID:
18662872
2.

Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.

Westaway SM, Thompson M, Rami HK, Stemp G, Trouw LS, Mitchell DJ, Seal JT, Medhurst SJ, Lappin SC, Biggs J, Wright J, Arpino S, Jerman JC, Cryan JE, Holland V, Winborn KY, Coleman T, Stevens AJ, Davis JB, Gunthorpe MJ.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5609-13. doi: 10.1016/j.bmcl.2008.08.105.

PMID:
18809327
3.

Spiro-piperidine azetidinones as potent TRPV1 antagonists.

Xiao D, Palani A, Aslanian R, McKittrick BA, McPhail AT, Correll CC, Phelps PT, Anthes JC, Rindgen D.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):783-7. doi: 10.1016/j.bmcl.2008.12.024.

PMID:
19114307
4.

From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.

Zheng X, Hodgetts KJ, Brielmann H, Hutchison A, Burkamp F, Brian Jones A, Blurton P, Clarkson R, Chandrasekhar J, Bakthavatchalam R, De Lombaert S, Crandall M, Cortright D, Blum CA.

Bioorg Med Chem Lett. 2006 Oct 1;16(19):5217-21.

PMID:
16870426
5.

Discovery of piperidine carboxamide TRPV1 antagonists.

Cheung WS, Calvo RR, Tounge BA, Zhang SP, Stone DR, Brandt MR, Hutchinson T, Flores CM, Player MR.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4569-72. doi: 10.1016/j.bmcl.2008.07.035.

PMID:
18662879
6.

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.

PMID:
19231185
7.

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.

PMID:
18835163
8.

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 1;18(13):3778-82. doi: 10.1016/j.bmcl.2008.05.036.

PMID:
18515099
9.

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.

PMID:
19553115
10.

Design and characterization of a noncompetitive antagonist of the transient receptor potential vanilloid subunit 1 channel with in vivo analgesic and anti-inflammatory activity.

García-Martínez C, Fernández-Carvajal A, Valenzuela B, Gomis A, Van Den Nest W, Ferroni S, Carreño C, Belmonte C, Ferrer-Montiel A.

J Pain. 2006 Oct;7(10):735-46.

PMID:
17018334
11.

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.

PMID:
19500979
12.

Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.

Gomtsyan A, Bayburt EK, Keddy R, Turner SC, Jinkerson TK, Didomenico S, Perner RJ, Koenig JR, Drizin I, McDonald HA, Surowy CS, Honore P, Mikusa J, Marsh KC, Wetter JM, Faltynek CR, Lee CH.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3894-9.

PMID:
17507218
13.

Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.

Norman MH, Zhu J, Fotsch C, Bo Y, Chen N, Chakrabarti P, Doherty EM, Gavva NR, Nishimura N, Nixey T, Ognyanov VI, Rzasa RM, Stec M, Surapaneni S, Tamir R, Viswanadhan VN, Treanor JJ.

J Med Chem. 2007 Jul 26;50(15):3497-514.

PMID:
17585749
14.

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.

PMID:
22153342
15.

Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity.

Li Y, Liang J, Siu T, Hu E, Rossi MA, Barnett SF, Defeo-Jones D, Jones RE, Robinson RG, Leander K, Huber HE, Mittal S, Cosford N, Prasit P.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):834-6. doi: 10.1016/j.bmcl.2008.12.017.

PMID:
19097777
16.

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.

PMID:
18550373
17.

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.

PMID:
19500982
18.

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.

PMID:
22172695
19.

Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade.

Gavva NR, Bannon AW, Hovland DN Jr, Lehto SG, Klionsky L, Surapaneni S, Immke DC, Henley C, Arik L, Bak A, Davis J, Ernst N, Hever G, Kuang R, Shi L, Tamir R, Wang J, Wang W, Zajic G, Zhu D, Norman MH, Louis JC, Magal E, Treanor JJ.

J Pharmacol Exp Ther. 2007 Oct;323(1):128-37.

20.

Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.

Voight EA, Gomtsyan AR, Daanen JF, Perner RJ, Schmidt RG, Bayburt EK, DiDomenico S, McDonald HA, Puttfarcken PS, Chen J, Neelands TR, Bianchi BR, Han P, Reilly RM, Franklin PH, Segreti JA, Nelson RA, Su Z, King AJ, Polakowski JS, Baker SJ, Gauvin DM, Lewis LR, Mikusa JP, Joshi SK, Faltynek CR, Kym PR, Kort ME.

J Med Chem. 2014 Sep 11;57(17):7412-24. doi: 10.1021/jm500916t.

PMID:
25100568
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