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  3. Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics

Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics

  • Bioorg Med Chem Lett. 2012 Jan 1;22(1):461-7. doi: 10.1016/j.bmcl.2011.10.104.
Rogier A Smits 1,  Herman D Lim,  Tiffany van der Meer,  Sebastiaan Kuhne,  Karin Bessembinder,  Obbe P Zuiderveld,  Maikel Wijtmans,  Iwan J P de Esch,  Rob Leurs
Affiliations

Affiliation

  • 1 Griffin Discoveries BV, Department of Medicinal Chemistry, Room P-246, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands.
PMID: 22153663 DOI: 10.1016/j.bmcl.2011.10.104
Abstract

The histamine H(4) receptor is a G protein-coupled receptor that has attracted much interest for its role in inflammatory and immunomodulatory functions. In our search for new H(4)R ligands, a low affinity isoquinoline fragment was optimized to 7-(furan-2-yl)-4-(piperazin-1-yl)quinazolin-2-amine (VUF11489), as a new H(4)R antagonist. Analysis of its binding kinetics at the human H(4)R showed this compound to have a very different dissociative half-life in comparison with reference antagonist JNJ7777120.

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