de Esch IJ - Search Results

1

Surface plasmon resonance biosensor based fragment screening using acetylcholine binding protein identifies ligand efficiency hot spots (LE hot spots) by deconstruction of nicotinic acetylcholine receptor α7 ligands.

de Kloe GE, Retra K, Geitmann M, Källblad P, Nahar T, van Elk R, Smit AB, van Muijlwijk-Koezen JE, Leurs R, Irth H, Danielson UH, de Esch IJ. de Kloe GE, et al. Among authors: de esch ij. J Med Chem. 2010 Oct 14;53(19):7192-201. doi: 10.1021/jm100834y. J Med Chem. 2010. PMID: 20828128

2

Characterization of the binding site of the histamine H3 receptor. 1. Various approaches to the synthesis of 2-(1H-imidazol-4-yl)cyclopropylamine and histaminergic activity of (1R,2R)- and (1S,2S)-2-(1H-imidazol-4-yl)-cyclopropylamine.

De Esch IJ, Vollinga RC, Goubitz K, Schenk H, Appelberg U, Hacksell U, Lemstra S, Zuiderveld OP, Hoffmann M, Leurs R, Menge WM, Timmerman H. De Esch IJ, et al. J Med Chem. 1999 Apr 8;42(7):1115-22. doi: 10.1021/jm9810912. J Med Chem. 1999. PMID: 10197956 Free article.

3

Synthesis and histamine H3 receptor activity of 4-(n-alkyl)-1H-imidazoles and 4-(omega-phenylalkyl)-1H-imidazoles.

De Esch IJ, Gaffar A, Menge WM, Timmerman H. De Esch IJ, et al. Bioorg Med Chem. 1999 Dec;7(12):3003-9. doi: 10.1016/s0968-0896(99)00253-9. Bioorg Med Chem. 1999. PMID: 10658607

4

Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE.

De Esch IJ, Mills JE, Perkins TD, Romeo G, Hoffmann M, Wieland K, Leurs R, Menge WM, Nederkoorn PH, Dean PM, Timmerman H. De Esch IJ, et al. J Med Chem. 2001 May 24;44(11):1666-74. doi: 10.1021/jm001109k. J Med Chem. 2001. PMID: 11356102

5

Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.

Kitbunnadaj R, Zuiderveld OP, De Esch IJ, Vollinga RC, Bakker R, Lutz M, Spek AL, Cavoy E, Deltent MF, Menge WM, Timmerman H, Leurs R. Kitbunnadaj R, et al. Among authors: de esch ij. J Med Chem. 2003 Dec 4;46(25):5445-57. doi: 10.1021/jm030905y. J Med Chem. 2003. PMID: 14640553

6

Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.

Terzioglu N, van Rijn RM, Bakker RA, De Esch IJ, Leurs R. Terzioglu N, et al. Among authors: de esch ij. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5251-6. doi: 10.1016/j.bmcl.2004.08.035. Bioorg Med Chem Lett. 2004. PMID: 15454206

7

The histamine H3 receptor: from gene cloning to H3 receptor drugs.

Leurs R, Bakker RA, Timmerman H, de Esch IJ. Leurs R, et al. Among authors: de esch ij. Nat Rev Drug Discov. 2005 Feb;4(2):107-20. doi: 10.1038/nrd1631. Nat Rev Drug Discov. 2005. PMID: 15665857 Review.

8

N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.

Kitbunnadaj R, Hashimoto T, Poli E, Zuiderveld OP, Menozzi A, Hidaka R, de Esch IJ, Bakker RA, Menge WM, Yamatodani A, Coruzzi G, Timmerman H, Leurs R. Kitbunnadaj R, et al. Among authors: de esch ij. J Med Chem. 2005 Mar 24;48(6):2100-7. doi: 10.1021/jm049475h. J Med Chem. 2005. PMID: 15771452

9

Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists.

Storelli S, Verdijk P, Verzijl D, Timmerman H, van de Stolpe AC, Tensen CP, Smit MJ, De Esch IJ, Leurs R. Storelli S, et al. Among authors: de esch ij. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2910-3. doi: 10.1016/j.bmcl.2005.03.070. Bioorg Med Chem Lett. 2005. PMID: 15911279

10

The histamine H4 receptor as a new therapeutic target for inflammation.

de Esch IJ, Thurmond RL, Jongejan A, Leurs R. de Esch IJ, et al. Trends Pharmacol Sci. 2005 Sep;26(9):462-9. doi: 10.1016/j.tips.2005.07.002. Trends Pharmacol Sci. 2005. PMID: 16054239 Review.

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