Leurs R - Search Results

1

Lead Optimization of the 5-Phenylpyrazolopyrimidinone NPD-2975 toward Compounds with Improved Antitrypanosomal Efficacy.

Zheng Y, van den Kerkhof M, Ibrahim M, De Esch IJP, Maes L, Sterk GJ, Caljon G, Leurs R. Zheng Y, et al. Among authors: leurs r. J Med Chem. 2024 Feb 22;67(4):2849-2863. doi: 10.1021/acs.jmedchem.3c01976. Epub 2024 Feb 8. J Med Chem. 2024. PMID: 38330051 Free PMC article.

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. Among authors: leurs r. 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. Among authors: leurs r. 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. Among authors: leurs r. 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. Among authors: leurs r. 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. Among authors: leurs r. 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. Among authors: leurs r. 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. Among authors: leurs r. 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. Among authors: leurs r. J Med Chem. 2005 Oct 6;48(20):6461-71. doi: 10.1021/jm050418d. J Med Chem. 2005. PMID: 16190772

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