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Comparative Study
. 2004 Nov 1;14(21):5251-6.
doi: 10.1016/j.bmcl.2004.08.035.

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

Nalan Terzioglu  1 , Richard M van Rijn, Remko A Bakker, Iwan J P De Esch, Rob Leurs
Affiliations
Comparative Study

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

Nalan Terzioglu et al. Bioorg Med Chem Lett. .

Abstract

We describe the structure-activity relationships for a series of ligands structurally related to the recently identified (5-chloro-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanone (1) as histamine H(4) receptor (H(4)R) antagonists. Furthermore, we identified related benzimidazoles as novel lead compounds for the H(4)R. The ligands have been evaluated by radioligand displacement studies and functional assays for their interaction with both the human histamine H(3) and H(4) receptors and exhibit pK(i) values up to 7.5 at the human H(4)R.

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