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

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.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2008, Vol.18 (1), p.39-43
Hauptverfasser:	LY, Kiev S, LETAVIC, Michael A, DVORAK, Lisa, MILLER, Kirsten L, NEPOMUCENO, Diane, WILSON, Sandy J, CARRUTHERS, Nicholas I, KEITH, John M, MILLER, Jennifer M, STOCKING, Emily M, BARBIER, Ann J, BONAVENTURE, Pascal, LORD, Brian, XIAOHUI JIANG, BOGGS, Jamin D
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemical synthesis Amides - pharmacokinetics Amides - pharmacology Animals Azepines - chemical synthesis Azepines - pharmacokinetics Azepines - pharmacology Biological and medical sciences Brain - metabolism Histamine H3 Antagonists - chemical synthesis Histamine H3 Antagonists - pharmacokinetics Histamine H3 Antagonists - pharmacology Humans Medical sciences Neuropharmacology Pharmacology. Drug treatments Piperazines - chemical synthesis Piperazines - pharmacokinetics Piperazines - pharmacology Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology Rats Serotonin Uptake Inhibitors - chemical synthesis Serotonin Uptake Inhibitors - pharmacokinetics Serotonin Uptake Inhibitors - pharmacology Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.11.016