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Items: 1 to 20 of 110

1.

Optimisation of imidazole compounds as selective TAAR1 agonists: discovery of RO5073012.

Galley G, Stalder H, Goergler A, Hoener MC, Norcross RD.

Bioorg Med Chem Lett. 2012 Aug 15;22(16):5244-8. doi: 10.1016/j.bmcl.2012.06.060. Epub 2012 Jun 23.

PMID:
22795332
2.

Design and synthesis of imidazoline derivatives active on glucose homeostasis in a rat model of type II diabetes. 2. Syntheses and biological activities of 1,4-dialkyl-, 1,4-dibenzyl, and 1-benzyl-4-alkyl-2-(4',5'-dihydro-1'H-imidazol-2'-yl)piperazines and isosteric analogues of imidazoline.

Le Bihan G, Rondu F, Pelé-Tounian A, Wang X, Lidy S, Touboul E, Lamouri A, Dive G, Huet J, Pfeiffer B, Renard P, Guardiola-Lemaître B, Manéchez D, Pénicaud L, Ktorza A, Godfroid JJ.

J Med Chem. 1999 May 6;42(9):1587-603.

3.

Receptor-specific functional efficacies of alkyl imidazoles as dual histamine H3/H4 receptor ligands.

Kottke T, Sander K, Weizel L, Schneider EH, Seifert R, Stark H.

Eur J Pharmacol. 2011 Mar 11;654(3):200-8. doi: 10.1016/j.ejphar.2010.12.033. Epub 2011 Jan 13.

PMID:
21237145
4.

Pharmacologic characterization of the cloned human trace amine-associated receptor1 (TAAR1) and evidence for species differences with the rat TAAR1.

Wainscott DB, Little SP, Yin T, Tu Y, Rocco VP, He JX, Nelson DL.

J Pharmacol Exp Ther. 2007 Jan;320(1):475-85. Epub 2006 Oct 12.

5.
6.

Trace amine-associated receptor 1 partial agonism reveals novel paradigm for neuropsychiatric therapeutics.

Revel FG, Moreau JL, Gainetdinov RR, Ferragud A, Velázquez-Sánchez C, Sotnikova TD, Morairty SR, Harmeier A, Groebke Zbinden K, Norcross RD, Bradaia A, Kilduff TS, Biemans B, Pouzet B, Caron MG, Canales JJ, Wallace TL, Wettstein JG, Hoener MC.

Biol Psychiatry. 2012 Dec 1;72(11):934-42. doi: 10.1016/j.biopsych.2012.05.014. Epub 2012 Jun 16.

PMID:
22705041
7.

Synthesis and evaluation of potent and selective beta(3) adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres.

Uehling DE, Donaldson KH, Deaton DN, Hyman CE, Sugg EE, Barrett DG, Hughes RG, Reitter B, Adkison KK, Lancaster ME, Lee F, Hart R, Paulik MA, Sherman BW, True T, Cowan C.

J Med Chem. 2002 Jan 31;45(3):567-83.

PMID:
11806709
8.

Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773).

Stalder H, Hoener MC, Norcross RD.

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1227-31. doi: 10.1016/j.bmcl.2010.12.075. Epub 2010 Dec 21.

PMID:
21237643
9.

Development of potent and selective small-molecule human Urotensin-II antagonists.

McAtee JJ, Dodson JW, Dowdell SE, Girard GR, Goodman KB, Hilfiker MA, Sehon CA, Sha D, Wang GZ, Wang N, Viet AQ, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Yuan CC, Douglas SA, Neeb MJ.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3500-3. doi: 10.1016/j.bmcl.2008.05.027. Epub 2008 May 10.

PMID:
18502123
10.

Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines.

Hodson SJ, Bigham EC, Garrison DT, Gobel MJ, Irving PE, Liacos JA, Navas F 3rd, Saussy DL Jr, Sherman BW, Speake JD, Bishop MJ.

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3449-52.

PMID:
12419381
11.

Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series.

Barlaam B, Ducray R, Lambert-van der Brempt C, Plé P, Bardelle C, Brooks N, Coleman T, Cross D, Kettle JG, Read J.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2207-11. doi: 10.1016/j.bmcl.2011.03.009.

PMID:
21441027
12.

Discovery and optimization of arylsulfonyl 3-(pyridin-2-yloxy)anilines as novel GPR119 agonists.

Zhang JK, Li AR, Yu M, Wang Y, Zhu J, Kayser F, Medina JC, Siegler K, Conn M, Shan B, Grillo MP, Eksterowicz J, Coward P, Liu JJ.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3609-13. doi: 10.1016/j.bmcl.2013.04.014. Epub 2013 Apr 15.

PMID:
23648181
13.

Design and synthesis of novel imidazole-substituted dipeptide amides as potent and selective inhibitors of Candida albicans myristoylCoA:protein N-myristoyltransferase and identification of related tripeptide inhibitors with mechanism-based antifungal activity.

Devadas B, Freeman SK, Zupec ME, Lu HF, Nagarajan SR, Kishore NS, Lodge JK, Kuneman DW, McWherter CA, Vinjamoori DV, Getman DP, Gordon JI, Sikorski JA.

J Med Chem. 1997 Aug 1;40(16):2609-25.

PMID:
9258368
14.

Identification of a novel, orally bioavailable histamine H(3) receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template.

Aslanian R, Mutahi MW, Shih NY, McCormick KD, Piwinski JJ, Ting PC, Albanese MM, Berlin MY, Zhu X, Wong SC, Rosenblum SB, Jiang Y, West R, She S, Williams SM, Bryant M, Hey JA.

Bioorg Med Chem Lett. 2002 Mar 25;12(6):937-41.

PMID:
11958998
15.

A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors.

Hong SS, Romstedt KJ, Feller DR, Hsu FL, Cupps TL, Lyon RA, Miller DD.

J Med Chem. 1994 Jul 22;37(15):2328-33.

PMID:
7914537
16.

N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.

Igel P, Schneider E, Schnell D, Elz S, Seifert R, Buschauer A.

J Med Chem. 2009 Apr 23;52(8):2623-7. doi: 10.1021/jm9000693.

PMID:
19317445
17.

Structure-activity relationships of 2,4-diphenyl-1H-imidazole analogs as CB2 receptor agonists for the treatment of chronic pain.

Yang SW, Smotryski J, Matasi J, Ho G, Tulshian D, Greenlee WJ, Brusa R, Beltramo M, Cox K.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):182-5. doi: 10.1016/j.bmcl.2010.11.044. Epub 2010 Nov 11.

PMID:
21115245
18.

Synthesis and biological evaluation of imidazole derivatives as novel NOP/ORL1 receptor antagonists: exploration and optimization of alternative pyrazole structure.

Sugimoto Y, Kobayashi K, Asai M, Ohno A, Yamada K, Ozaki S, Ohta H, Okamoto O.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4611-6. doi: 10.1016/j.bmcl.2009.06.095. Epub 2009 Jul 1.

PMID:
19604695
19.

Synthesis and serotonergic activity of substituted 2, N-benzylcarboxamido-5-(2-ethyl-1-dioxoimidazolidinyl)-N, N-dimethyltryptamine derivatives: novel antagonists for the vascular 5-HT(1B)-like receptor.

Moloney GP, Martin GR, Mathews N, Milne A, Hobbs H, Dodsworth S, Sang PY, Knight C, Williams M, Maxwell M, Glen RC.

J Med Chem. 1999 Jul 15;42(14):2504-26.

PMID:
10411472
20.

Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.

Liverton NJ, Butcher JW, Claiborne CF, Claremon DA, Libby BE, Nguyen KT, Pitzenberger SM, Selnick HG, Smith GR, Tebben A, Vacca JP, Varga SL, Agarwal L, Dancheck K, Forsyth AJ, Fletcher DS, Frantz B, Hanlon WA, Harper CF, Hofsess SJ, Kostura M, Lin J, Luell S, O'Neill EA, O'Keefe SJ, et al.

J Med Chem. 1999 Jun 17;42(12):2180-90.

PMID:
10377223

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