Triamino pyrimidines and pyridines as histamine H(4) receptor modulators

Steven P Meduna; Brad M Savall; Hui Cai; James P Edwards; Robin L Thurmond; Patricia M McGovern

doi:10.1016/j.bmcl.2011.03.017

Triamino pyrimidines and pyridines as histamine H(4) receptor modulators

Bioorg Med Chem Lett. 2011 May 15;21(10):3113-6. doi: 10.1016/j.bmcl.2011.03.017. Epub 2011 Mar 30.

Authors

Steven P Meduna¹, Brad M Savall, Hui Cai, James P Edwards, Robin L Thurmond, Patricia M McGovern

Affiliation

¹ Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. smeduna@its.jnj.com

PMID: 21458260
DOI: 10.1016/j.bmcl.2011.03.017

Abstract

Two series of triamino pyrimidines and a series of triamino pyridines have been synthesized and their structure-activity relationships evaluated for activity at the H(4) receptor in competitive binding and functional assays. Small structural changes in these three hetereoaromatic cores influenced the functional activity of these compounds.

MeSH terms

Amines / chemistry
Binding, Competitive
Biological Assay
Humans
Inhibitory Concentration 50
Molecular Structure
Protein Binding / drug effects
Pyridines / chemical synthesis
Pyridines / chemistry
Pyridines / pharmacology*
Pyrimidines / chemical synthesis
Pyrimidines / chemistry
Pyrimidines / pharmacology*
Receptors, G-Protein-Coupled / antagonists & inhibitors*
Receptors, Histamine
Receptors, Histamine H4
Structure-Activity Relationship

Substances

Amines
HRH4 protein, human
Pyridines
Pyrimidines
Receptors, G-Protein-Coupled
Receptors, Histamine
Receptors, Histamine H4