de Esch IJP - Search Results

1

4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H₃ Receptor Agonists with in Vivo Central Nervous System Activity.

Wágner G, Mocking TAM, Arimont M, Provensi G, Rani B, Silva-Marques B, Latacz G, Da Costa Pereira D, Karatzidou C, Vischer HF, Wijtmans M, Kieć-Kononowicz K, de Esch IJP, Leurs R. Wágner G, et al. Among authors: de esch ijp. J Med Chem. 2019 Dec 12;62(23):10848-10866. doi: 10.1021/acs.jmedchem.9b01462. Epub 2019 Nov 20. J Med Chem. 2019. PMID: 31675226 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. 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

A qualitative model for the histamine H3 receptor explaining agonistic and antagonistic activity simultaneously.

de Esch IJ, Timmerman H, Menge WM, Nederkoorn PH. de Esch IJ, et al. Arch Pharm (Weinheim). 2000 Aug;333(8):254-60. doi: 10.1002/1521-4184(20008)333:8<254::aid-ardp254>3.0.co;2-g. Arch Pharm (Weinheim). 2000. PMID: 11008375

5

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

6

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

7

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

8

Histamine H3 receptor agonists.

De Esch IJ, Belzar KJ. De Esch IJ, et al. Mini Rev Med Chem. 2004 Nov;4(9):955-63. doi: 10.2174/1389557043403134. Mini Rev Med Chem. 2004. PMID: 15544556 Review.

9

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.

10

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

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