de Esch IJP - Search Results

1

Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists.

Adlere I, Sun S, Zarca A, Roumen L, Gozelle M, Viciano CP, Caspar B, Arimont M, Bebelman JP, Briddon SJ, Hoffmann C, Hill SJ, Smit MJ, Vischer HF, Wijtmans M, de Graaf C, de Esch IJP, Leurs R. Adlere I, et al. Among authors: de graaf c, de esch ijp. Eur J Med Chem. 2019 Jan 15;162:631-649. doi: 10.1016/j.ejmech.2018.10.060. Epub 2018 Oct 30. Eur J Med Chem. 2019. PMID: 30476826

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

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

4

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. J Med Chem. 2003 Dec 4;46(25):5445-57. doi: 10.1021/jm030905y. J Med Chem. 2003. PMID: 14640553

5

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. 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

6

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

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

7

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. J Med Chem. 2005 Mar 24;48(6):2100-7. doi: 10.1021/jm049475h. J Med Chem. 2005. PMID: 15771452

8

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. 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

9

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.

10

Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human cytomegalovirus encoded chemokine receptor US28.

Hulshof JW, Casarosa P, Menge WM, Kuusisto LM, van der Goot H, Smit MJ, de Esch IJ, Leurs R. Hulshof JW, et al. J Med Chem. 2005 Oct 6;48(20):6461-71. doi: 10.1021/jm050418d. J Med Chem. 2005. PMID: 16190772

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