Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors

Kiev S Ly; Michael A Letavic; John M Keith; Jennifer M Miller; Emily M Stocking; Ann J Barbier; Pascal Bonaventure; Brian Lord; Xiaohui Jiang; Jamin D Boggs; Lisa Dvorak; Kirsten L Miller; Diane Nepomuceno; Sandy J Wilson; Nicholas I Carruthers

doi:10.1016/j.bmcl.2007.11.016

Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors

Bioorg Med Chem Lett. 2008 Jan 1;18(1):39-43. doi: 10.1016/j.bmcl.2007.11.016. Epub 2007 Nov 13.

Authors

Kiev S Ly¹, Michael A Letavic, John M Keith, Jennifer M Miller, Emily M Stocking, Ann J Barbier, Pascal Bonaventure, Brian Lord, Xiaohui Jiang, Jamin D Boggs, Lisa Dvorak, Kirsten L Miller, Diane Nepomuceno, Sandy J Wilson, Nicholas I Carruthers

Affiliation

¹ Johnson & Johnson Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.

PMID: 18060777
DOI: 10.1016/j.bmcl.2007.11.016

Abstract

The synthesis and biological activity of a new series of piperazine and diazepane amides is described. The new compounds are high affinity histamine H3 ligands and serotonin reuptake inhibitors.

MeSH terms

Amides / chemical synthesis
Amides / pharmacokinetics
Amides / pharmacology
Animals
Azepines / chemical synthesis*
Azepines / pharmacokinetics
Azepines / pharmacology
Brain / metabolism
Histamine H3 Antagonists / chemical synthesis*
Histamine H3 Antagonists / pharmacokinetics
Histamine H3 Antagonists / pharmacology
Humans
Piperazines / chemical synthesis*
Piperazines / pharmacokinetics
Piperazines / pharmacology
Rats
Selective Serotonin Reuptake Inhibitors / chemical synthesis*
Selective Serotonin Reuptake Inhibitors / pharmacokinetics
Selective Serotonin Reuptake Inhibitors / pharmacology
Structure-Activity Relationship

Substances

Amides
Azepines
Histamine H3 Antagonists
Piperazines
Serotonin Uptake Inhibitors