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Inflammation Research
Published in: Inflammation Research 2/2010

01-03-2010 | Short Communication

Lead identification and optimization of diaminopyrimidines as histamine H4 receptor ligands

Authors: K. Sander, T. Kottke, E. Proschak, Y. Tanrikulu, E. H. Schneider, R. Seifert, G. Schneider, H. Stark

Published in: Inflammation Research | Special Issue 2/2010

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Abstract

Background

The human histamine H4 receptor (hH4R) is a promising new target in the therapy of inflammatory or immune system diseases.

Methods

For the development of new hH4R ligands, a broad virtual screening was performed and two hits were identified. Their annelated heterocyclic core was optimized with regard to affinity and potency.

Results

Pharmacological characterization of the resulting diaminopyrimidines revealed different agonist and antagonist properties within the same scaffold.
Literature
1.
Zampeli E, Tiligada E. The role of histamine H4 receptor in immune and inflammatory disorders. Br J Pharmacol. 2009;157:24–33.CrossRefPubMed
2.
Kiss R, Keserü GM. Histamine H4 receptor ligands and their potential therapeutic applications. Expert Opin Ther Pat. 2009;19:119–35.CrossRefPubMed
3.
Schneider G, Neidhart W, Giller T, Schmid G. “Scaffold-hopping” by topological pharmacophore search: a contribution to virtual screening. Angew Chem Int Ed. 1999;38:2894–6.CrossRef
4.
Schneider EH, Schnell D, Papa D, Seifert R. High constitutive activity and a G protein-independent high-affinity state of the human histamine H4 receptor. Biochemistry. 2009;48:1424–38.CrossRefPubMed
5.
Rodionov VO, Fokin VV, Finn MG. Mechanism of the ligand-free Cu(I)-catalyzed azide-alkyne cycloaddition reaction. Angew Chem Int Ed. 2005;44:2210–5.CrossRef
6.
Luo G, Chen L, Poindexter GS. Microwave-assisted synthesis of aminopyrimidines. Tetrahedron Lett. 2002;43:5739–42.CrossRef
7.
Tanrikulu Y, Proschak E, Werner T, Geppert T, Todoroff N, Klenner A, et al. Homology model adjustment and ligand screening with a pseudoreceptor of the human histamine H4 receptor. ChemMedChem. 2009;4:820–7.CrossRefPubMed
Metadata
Title
Lead identification and optimization of diaminopyrimidines as histamine H4 receptor ligands
Authors
K. Sander
T. Kottke
E. Proschak
Y. Tanrikulu
E. H. Schneider
R. Seifert
G. Schneider
H. Stark
Publication date
01-03-2010
Publisher
SP Birkhäuser Verlag Basel
Published in
Inflammation Research / Issue Special Issue 2/2010
Print ISSN: 1023-3830
Electronic ISSN: 1420-908X
DOI
https://doi.org/10.1007/s00011-009-0143-2

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